Zonisamide

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Identification

Summary

Zonisamide is a sulfonamide anticonvulsant used to treat partial seizures.

Brand Names

Zonegran, Zonisade

Generic Name

Zonisamide

DrugBank Accession Number

DB00909

Background

Zonisamide is a sulfonamide anticonvulsant used as an adjunctive therapy in adults with partial-onset seizures.^7,8 Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels, leading to a reduction of T-type calcium channel currents or by binding allosterically to GABA receptors. This latter action may inhibit the uptake of the inhibitory neurotransmitter GABA while enhancing the uptake of the excitatory neurotransmitter glutamate.^7,8 Zonisamide represents an alternative for patients that remain refractory to established antiepileptic drugs. In 1989, it was approved for commercial use in Japan. The US and Europe approved it in 2000 and 2005, respectively.^1,4

Type

Small Molecule

Groups

Approved, Investigational

Structure

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Zonisamide (DB00909)

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Weight

Average: 212.226
Monoisotopic: 212.025562822

Chemical Formula

C₈H₈N₂O₃S

Synonyms

• 1,2-Benzisoxazole-3-methanesulfonamide
• 3-(Sulfamoylmethyl)-1,2-benzisoxazole
• Benzo[d]isoxazol-3-yl-methanesulfonamide
• Zonisamida
• Zonisamide
• Zonisamidum

External IDs

• AD-810
• CI-912
• PD-110843

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Pharmacology

Indication

Zonisamide capsules are indicated as adjunctive therapy in the treatment of partial seizures in adults with epilepsy.⁷ Zonisamide oral suspension is indicated as adjunctive therapy for the treatment of partial-onset seizures in adults and pediatric patients 16 years of age and older.⁸

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Adjunct therapy in treatment of	Partial-onset seizures		••••••••••••	•••••		•••••••
Adjunct therapy in treatment of	Partial-onset seizures		••••••••••••			••••••••••

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Pharmacodynamics

By stopping the spread of seizure discharges, zonisamide prevents the extensor component of tonic convulsion, restricts the spread of focal seizures and prevents the propagation of seizures from the cortex to subcortical structures.^4,5 In animal models, zonisamide was effective against tonic extension seizures but ineffective against clonic seizures. It also increased the threshold for generalized seizures and reduced the duration of cortical focal seizures.⁷ Aside from its antiepileptic effects, zonisamide is capable of activating neuroprotective mechanisms. It inhibits nitric oxide synthase and ​​reduces ischemia-induced memory impairment and lipid peroxidation.⁴

The use of zonisamide may lead to potentially fatal reactions. Severe reactions such as Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, and aplastic anemia have been reported in patients treated with sulfonamides such as zonisamide. Zonisamide may also lead to the development of serious hematological events, drug reaction with eosinophilia and systemic symptoms (DRESS) and multi-organ hypersensitivity, acute myopia and secondary angle closure glaucoma, as well as suicidal behaviour and ideation.^7,8 Zonisamide is a carbonic anhydrase inhibitor, which may lead to metabolic acidosis in patients treated with this drug. Its therapeutic effects due to this pharmacological action are unknown.⁷

Mechanism of action

The mechanism of action by which zonisamide controls seizures has not been fully established. However, its antiepileptic properties may be due to its effects on sodium and calcium channels.^7,8 Zonisamide blocks sodium channels and reduces voltage-dependent, transient inward currents, stabilizing neuronal membranes and suppressing neuronal hypersynchronization.^7,8 It affects T-type calcium currents, but has no effect on L-type calcium currents.^3,4,6

Zonisamide suppresses synaptically-driven electrical activity by altering the synthesis, release, and degradation of neurotransmitters, such as glutamate, gamma-aminobutyric acid (GABA), dopamine, serotonin (5-hydroxytryptamine 5-HT), and acetylcholine.^4,2 Furthermore, it binds to the GABA/benzodiazepine receptor ionophore complex without producing changes in chloride flux.^7,8 In vitro studies have suggested that zonisamide does not affect postsynaptic GABA or glutamate responses, nor the neuronal or glial uptake of [³H]-GABA.

Target	Actions	Organism
ASodium channel protein type 1 subunit alpha	inhibitor	Humans
ASodium channel protein type 2 subunit alpha	inhibitor	Humans
ASodium channel protein type 3 subunit alpha	inhibitor	Humans
ASodium channel protein type 4 subunit alpha	inhibitor	Humans
ASodium channel protein type 5 subunit alpha	inhibitor	Humans
ASodium channel protein type 9 subunit alpha	inhibitor	Humans
ASodium channel protein type 11 subunit alpha	inhibitor	Humans
ASodium channel subunit beta-1	inhibitor	Humans
ASodium channel subunit beta-2	inhibitor	Humans
ASodium channel regulatory subunit beta-3	inhibitor	Humans
ASodium channel subunit beta-4	inhibitor	Humans
AVoltage-dependent T-type calcium channel subunit alpha-1G	inhibitor	Humans
AVoltage-dependent T-type calcium channel subunit alpha-1H	inhibitor	Humans
AVoltage-dependent T-type calcium channel subunit alpha-1I	inhibitor	Humans
UCarbonic anhydrase 1	inhibitor	Humans
UCarbonic anhydrase 2	inhibitor	Humans
UCarbonic anhydrase 3	inhibitor	Humans
UCarbonic anhydrase 4	inhibitor	Humans
UCarbonic anhydrase 5A, mitochondrial	inhibitor	Humans
UCarbonic anhydrase 5B, mitochondrial	inhibitor	Humans
UCarbonic anhydrase 6	inhibitor	Humans
UCarbonic anhydrase 7	inhibitor	Humans
UCarbonic anhydrase-related protein	inhibitor	Humans
UCarbonic anhydrase 9	inhibitor	Humans
UCarbonic anhydrase-related protein 10	inhibitor	Humans
UCarbonic anhydrase-related protein 11	inhibitor	Humans
UCarbonic anhydrase 12	inhibitor	Humans
UCarbonic anhydrase 13	inhibitor	Humans
UCarbonic anhydrase 14	inhibitor	Humans
UAmine oxidase [flavin-containing] B	inhibitor	Humans
UAmine oxidase [flavin-containing] A	inhibitor	Humans
UGABA(A) Receptor Benzodiazepine Binding Site	binder	Humans

Absorption

Between 200 and 400 mg, zonisamide follows a dose-proportional pharmacokinetic profile.^7,8 At concentrations higher than 800 mg, the C_max and AUC increase in a disproportional manner, possibly due to zonisamide binding red blood cells. In healthy volunteers given 200 to 400 mg of zonisamide orally, peak plasma concentrations (C_max) range between 2 and 5 µg/mL and are reached within 2–6 hours (T_max).⁷ In healthy volunteers given 100 mg of zonisamide oral suspension, the T_max ranged from 0.5 to 5 hours.⁸ Zonisamide has a high oral bioavailability (95%).⁴ The T_max of zonisamide was delayed by food intake (4-6 hours); however, food has no effect on its bioavailability. Steady state is achieved 14 days after a stable dose is reached.^7,8

Volume of distribution

Following a 400 mg oral dose, zonisamide has an apparent volume of distribution (V/F) of 1.45 L/kg.^7,8

Protein binding

At concentrations between 1.0 and 7.0 μg/mL, zonisamide is approximately 40% bound to human plasma proteins.^7,8 The concentration of zonisamide is 8-fold higher in red blood cells than in plasma due to its ability to bind extensively to erythrocytes. The presence of therapeutic concentrations of phenytoin, phenobarbital, or carbamazepine does not affect zonisamide protein binding.^7,8

Metabolism

Zonisamide metabolites are generated mainly by principally reductive and conjugative mechanisms. Oxidation reactions play a minor role in the metabolism of zonisamide.⁴ Zonisamide is metabolized by N-acetyl-transferases to form N-acetyl zonisamide and reduced to form the open ring metabolite, 2–sulfamoylacetylphenol (SMAP). The reduction of zonisamide to SMAP is mediated by CYP3A4.^1,4,7,8 Zonisamide does not induce liver enzymes or its own metabolism.¹

Hover over products below to view reaction partners

• Zonisamide
  • 2-sulfamoylacetylphenol
  • N-acetyl zonisamide

Route of elimination

Zonisamide is mainly excreted as the parent drug and the glucuronide of a metabolite. Urine is the main route of zonisamide excretion, and only a small portion of this drug is excreted in feces.¹ Following multiple doses of radiolabeled zonisamide, 62% of the dose was recovered in the urine, and 3% in feces by day 10. Of the excreted dose of zonisamide, 35% was recovered unchanged, 15% as N-acetyl zonisamide, and 50% as the glucuronide of 2–sulfamoylacetylphenol (SMAP).^7,8

Half-life

In plasma, the elimination half-life of zonisamide is approximately 63 hours. In red blood cells, it is approximately 105 hours.^7,8

Clearance

In patients not taking enzyme-inducing antiepilepsy drugs (AEDs), the plasma clearance of oral zonisamide is approximately 0.30-0.35 mL/min/kg. In patients treated with AEDs, this value increases to 0.5 mL/min/kg.^7,8 Renal clearance is approximately 3.5 mL/min after a single-dose of zonisamide.^7,8 In red blood cells, the clearance of an oral dose of zonisamide is 2 mL/min.⁷

Adverse Effects

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Toxicity

Information on daily doses over 800 mg/day of zonisamide is limited. During clinical development, three patients ingested unknown amounts of zonisamide as suicide attempts, and all of them were hospitalized with central nervous system symptoms. One patient became comatose and developed bradycardia, hypotension, and respiratory depression; 31 hours after zonisamide ingestion, plasma level was 100.1 µg/mL. Zonisamide plasma levels fell with a half-life of 57 hours, and the patient became alert five days later.^7,8 There are no specific antidotes for zonisamide overdosage. In case of a suspected recent overdose, emesis should be induced or gastric lavage performed with the usual precautions to protect the airway. General supportive care is indicated, including frequent monitoring of vital signs and close observation.^7,8 Due to its long half-life and low protein binding, renal dialysis may be effective in treating zonisamide overdose; however, the effectiveness of this procedure has not been formally studied.⁸

In vivo studies found no evidence of carcinogenicity at zonisamide doses equivalent to or higher than the maximum recommended human dose (MRHD). In an in vitro chromosomal aberration assay in CHL cells, zonisamide displayed mutagenicity. Signs of reproductive toxicity were also detected in rats treated with a dose 0.5 times the MRHD.^7,8

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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1,2-Benzodiazepine	The risk or severity of CNS depression can be increased when Zonisamide is combined with 1,2-Benzodiazepine.
Abacavir	Zonisamide may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abametapir	The serum concentration of Zonisamide can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Zonisamide can be increased when combined with Abatacept.
Abemaciclib	The serum concentration of Abemaciclib can be increased when it is combined with Zonisamide.

Food Interactions

• Avoid alcohol. Ingesting alcohol may increase drowsiness and dizziness.
• Take with or without food.

Products

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International/Other Brands

Exceglan / Excegram

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Zonegran	Capsule	100 mg	Oral	Amdipharm Limited	2016-09-20	Not applicable
Zonegran	Capsule	100 mg	Oral	Amdipharm Limited	2016-09-20	Not applicable
Zonegran	Tablet, orally disintegrating	50 mg	Oral	Amdipharm Limited	2016-09-20	2020-02-07
Zonegran	Capsule	25 mg	Oral	Amdipharm Limited	2016-09-20	Not applicable
Zonegran	Capsule	25 mg	Oral	Amdipharm Limited	2016-09-20	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Zonisamide	Capsule	100 mg/1	Oral	Glenmark Pharmaceuticals Inc., USA	2006-01-30	Not applicable
Zonisamide	Capsule	50 mg/1	Oral	Dr.Reddy's Laboratories Limited	2005-12-22	2010-05-31
Zonisamide	Capsule	100 mg/1	Oral	Aidarex Pharmaceuticals LLC	2016-07-13	Not applicable
Zonisamide	Capsule	100 mg/1	Oral	Sun Pharmaceutical Industries, Inc.	2006-03-17	Not applicable
Zonisamide	Capsule	25 mg/1	Oral	PD-Rx Pharmaceuticals, Inc.	2005-12-23	2020-01-22

Categories

ATC Codes

N03AX15 — Zonisamide

• N03AX — Other antiepileptics
• N03A — ANTIEPILEPTICS
• N03 — ANTIEPILEPTICS
• N — NERVOUS SYSTEM

G01AE10 — Combinations of sulfonamides

• G01AE — Sulfonamides
• G01A — ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS
• G01 — GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS
• G — GENITO URINARY SYSTEM AND SEX HORMONES

Drug Categories

• Agents causing hyperkalemia
• Amides
• Anti-epileptic Agent
• Antiarrhythmic agents
• Anticonvulsants
• Bradycardia-Causing Agents
• Calcium Channel Blockers
• Calcium-Regulating Hormones and Agents
• Carbonic Anhydrase Inhibitors
• Cardiovascular Agents
• Central Nervous System Agents
• Central Nervous System Depressants
• Compounds used in a research, industrial, or household setting
• Cytochrome P-450 CYP2C19 Inhibitors
• Cytochrome P-450 CYP2C19 Inhibitors (weak)
• Cytochrome P-450 CYP2C19 Substrates
• Cytochrome P-450 CYP3A Substrates
• Cytochrome P-450 CYP3A4 Substrates
• Cytochrome P-450 CYP3A5 Substrates
• Cytochrome P-450 Enzyme Inhibitors
• Cytochrome P-450 Substrates
• Decreased Central Nervous System Disorganized Electrical Activity
• Diuretics
• Drugs that are Mainly Renally Excreted
• Isoxazoles
• Membrane Transport Modulators
• Monoamine Oxidase A Inhibitors for interaction with Monoamine Oxidase A substrates
• Nervous System
• P-glycoprotein inhibitors
• Potential QTc-Prolonging Agents
• QTc Prolonging Agents
• Sulfonamides
• Sulfones
• Sulfur Compounds
• UGT1A1 Substrates

Chemical TaxonomyProvided by Classyfire

Description

This compound belongs to the class of organic compounds known as benzisoxazoles. These are aromatic compounds containing a benzene ring fused to an isoxazole ring. Isoxazole is five-membered ring with three carbon atoms, and an oxygen atom next to a nitrogen atom.

Kingdom

Organic compounds

Super Class

Organoheterocyclic compounds

Class

Benzisoxazoles

Sub Class

Not Available

Direct Parent

Benzisoxazoles

Alternative Parents

Organosulfonamides / Organic sulfonamides / Benzenoids / Isoxazoles / Heteroaromatic compounds / Aminosulfonyl compounds / Oxacyclic compounds / Azacyclic compounds / Organopnictogen compounds / Organooxygen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives

show 3 more

Substituents

Aminosulfonyl compound / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzenoid / Benzisoxazole / Heteroaromatic compound / Hydrocarbon derivative / Isoxazole / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organic sulfonic acid amide / Organic sulfonic acid or derivatives / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Organosulfonic acid amide / Organosulfonic acid or derivatives / Organosulfur compound / Oxacycle / Sulfonyl

show 12 more

Molecular Framework

Aromatic heteropolycyclic compounds

External Descriptors

sulfonamide, 1,2-benzoxazoles (CHEBI:10127)

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

459384H98V

CAS number

68291-97-4

InChI Key

UBQNRHZMVUUOMG-UHFFFAOYSA-N

InChI

InChI=1S/C8H8N2O3S/c9-14(11,12)5-7-6-3-1-2-4-8(6)13-10-7/h1-4H,5H2,(H2,9,11,12)

IUPAC Name

(1,2-benzoxazol-3-yl)methanesulfonamide

SMILES

NS(=O)(=O)CC1=NOC2=CC=CC=C12

References

Synthesis Reference

Nidam, T. et al. Novel sulfonation method for zonisamide intermediate in zonisamide synthesis and their novel crystal forms. (2003) U.S. Patent US 2003/0144527 A1. Available at: https://patentimages.storage.googleapis.com/25/24/0f/19d95f38252d52/US20030144527A1.pdf

US20030114682

General References

1. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
2. Ueda Y, Doi T, Tokumaru J, Willmore LJ: Effect of zonisamide on molecular regulation of glutamate and GABA transporter proteins during epileptogenesis in rats with hippocampal seizures. Brain Res Mol Brain Res. 2003 Aug 19;116(1-2):1-6. [Article]
3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
4. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
5. Peters DH, Sorkin EM: Zonisamide. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in epilepsy. Drugs. 1993 May;45(5):760-87. [Article]
6. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
7. FDA Approved Drug Products: ZONEGRAN (zonisamide) capsules for oral use [Link]
8. FDA Approved Drug Products: ZONISADE (zonisamide) suspension for oral use [Link]

External Links

Human Metabolome Database

HMDB0015045

KEGG Drug

D00538

KEGG Compound

C07504

PubChem Compound

5734

PubChem Substance

46505278

ChemSpider

5532

BindingDB

50028010

RxNav

39998

ChEBI

10127

ChEMBL

CHEMBL750

ZINC

ZINC000000004321

Therapeutic Targets Database

DAP000500

PharmGKB

PA451978

PDBe Ligand

ZON

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

PDRhealth

PDRhealth Drug Page

Wikipedia

Zonisamide

PDB Entries

3po7

FDA label

Download (124 KB)

MSDS

Download (58.3 KB)

Clinical Trials

Clinical Trials

Clinical Trial & Rare Diseases Add-on Data Package

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Phase	Status	Purpose	Conditions	Count	Start Date	Why Stopped	100+ additional columns
Unlock 175K+ rows when you subscribe.View sample data
Not Available	Completed	Not Available	Epilepsy	2	somestatus	stop reason	just information to hide
Not Available	Completed	Not Available	Partial, Generalized and Combined Seizures	1	somestatus	stop reason	just information to hide
Not Available	Completed	Not Available	Partial-Onset Seizures	1	somestatus	stop reason	just information to hide
Not Available	Completed	Other	Alcohol Dependency	1	somestatus	stop reason	just information to hide
Not Available	Completed	Treatment	Obesity	1	somestatus	stop reason	just information to hide

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Pharmacoeconomics

Manufacturers

• Eisai inc
• Alphapharm party ltd
• Apotex inc etobicoke site
• Banner pharmacaps inc
• Barr laboratories inc
• Corepharma llc
• Dr reddys laboratories ltd
• Glenmark generics inc usa
• Invagen pharmaceuticals inc
• Mutual pharmaceutical co inc
• Mylan pharmaceuticals inc
• Roxane laboratories inc
• Sandoz inc
• Sun pharmaceutical industries ltd
• Teva pharmaceuticals usa
• Watson laboratories inc
• Wockhardt ltd
• Zydus pharmaceuticals usa inc

Packagers

• Alphapharm Party Ltd.
• Amerisource Health Services Corp.
• Apotex Inc.
• Barr Pharmaceuticals
• Bryant Ranch Prepack
• Corepharma LLC
• Diversified Healthcare Services Inc.
• Doctor Reddys Laboratories Ltd.
• Eisai Inc.
• Elan Pharmaceuticals Inc.
• Eon Labs
• Genpharm LP
• Glenmark Generics Ltd.
• Heartland Repack Services LLC
• InvaGen Pharmaceuticals Inc.
• Kaiser Foundation Hospital
• Lake Erie Medical and Surgical Supply
• Murfreesboro Pharmaceutical Nursing Supply
• Mylan
• Nucare Pharmaceuticals Inc.
• Physicians Total Care Inc.
• Ranbaxy Laboratories
• Rebel Distributors Corp.
• Resource Optimization and Innovation LLC
• Southwood Pharmaceuticals
• Stat Rx Usa
• Sun Pharmaceutical Industries Ltd.
• Teva Pharmaceutical Industries Ltd.
• UDL Laboratories
• Vangard Labs Inc.
• Wockhardt Ltd.

Dosage Forms

Form	Route	Strength
Capsule	Oral	25 mg
Tablet, orally disintegrating	Oral	100 mg
Tablet, orally disintegrating	Oral	25 mg
Tablet, orally disintegrating	Oral	300 mg
Tablet, orally disintegrating	Oral	50 mg
Tablet, coated	Oral	100 mg
Tablet, film coated	Oral	100 mg
Tablet	Oral	100 mg
Capsule	Oral	100 mg
Capsule	Oral	50 mg
Suspension	Oral	100 mg/5mL
Capsule	Oral	100 mg/1
Capsule	Oral	25 mg/1
Capsule	Oral	50 mg/1
Powder	Not applicable	1 g/1g
Capsule	Oral
Suspension	Oral	20 MG/ML

Prices

Unit description	Cost	Unit
Zonegran 100 mg capsule	3.33USD	capsule
Zonisamide 100 mg capsule	2.24USD	capsule
Zonegran 50 mg capsule	1.22USD	capsule
Zonisamide 50 mg capsule	1.12USD	capsule
Zonegran 25 mg capsule	0.94USD	capsule
Zonisamide 25 mg capsule	0.56USD	capsule

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US11478456	No	2018-08-18	2038-08-18
US11529333	No	2018-08-18	2038-08-18

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	161-163 °C	Dasgupta A. et al. Therapeutic Drug Monitoring Data: A Concise Guide. Academic Press, 2019, 4th edition.
water solubility	0.8 mg/mL	FDA Label
logP	0.5	Not Available
pKa	10.2	FDA Label

Predicted Properties

Property	Value	Source
Water Solubility	2.09 mg/mL	ALOGPS
logP	0.67	ALOGPS
logP	0.11	Chemaxon
logS	-2	ALOGPS
pKa (Strongest Acidic)	9.84	Chemaxon
pKa (Strongest Basic)	-1.7	Chemaxon
Physiological Charge	0	Chemaxon
Hydrogen Acceptor Count	3	Chemaxon
Hydrogen Donor Count	1	Chemaxon
Polar Surface Area	86.19 Å2	Chemaxon
Rotatable Bond Count	2	Chemaxon
Refractivity	50.3 m3·mol-1	Chemaxon
Polarizability	19.48 Å3	Chemaxon
Number of Rings	2	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	1.0
Blood Brain Barrier	+	0.9755
Caco-2 permeable	-	0.6385
P-glycoprotein substrate	Non-substrate	0.8681
P-glycoprotein inhibitor I	Non-inhibitor	0.9258
P-glycoprotein inhibitor II	Non-inhibitor	0.9513
Renal organic cation transporter	Non-inhibitor	0.8463
CYP450 2C9 substrate	Non-substrate	0.8828
CYP450 2D6 substrate	Non-substrate	0.9116
CYP450 3A4 substrate	Non-substrate	0.5419
CYP450 1A2 substrate	Non-inhibitor	0.5762
CYP450 2C9 inhibitor	Non-inhibitor	0.697
CYP450 2D6 inhibitor	Non-inhibitor	0.8081
CYP450 2C19 inhibitor	Non-inhibitor	0.6007
CYP450 3A4 inhibitor	Non-inhibitor	0.8141
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.7315
Ames test	Non AMES toxic	0.6276
Carcinogenicity	Non-carcinogens	0.7572
Biodegradation	Not ready biodegradable	0.9708
Rat acute toxicity	2.0592 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.8549
hERG inhibition (predictor II)	Non-inhibitor	0.8937

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	splash10-001i-1900000000-073e3341083b72e5e4ce
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	splash10-0gx0-0940000000-22533c93dd06de52f6a8
LC-MS/MS Spectrum - LC-ESI-QFT , negative	LC-MS/MS	splash10-014i-0900000000-c05ae650c884adcaba5a
LC-MS/MS Spectrum - LC-ESI-QFT , negative	LC-MS/MS	splash10-014i-0900000000-477908537d156d43e3a9
LC-MS/MS Spectrum - LC-ESI-QFT , negative	LC-MS/MS	splash10-014i-0900000000-f537644668fbc9b2e02b
LC-MS/MS Spectrum - LC-ESI-QFT , negative	LC-MS/MS	splash10-014i-1900000000-6359b9c8e68ec5477b26
LC-MS/MS Spectrum - LC-ESI-QFT , negative	LC-MS/MS	splash10-014i-3900000000-db3cf8881465259c48ca
LC-MS/MS Spectrum - LC-ESI-QFT , negative	LC-MS/MS	splash10-014i-6900000000-cd4c8b86f36ce38b3a49
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-0udi-0930000000-a0dd3941aea211aeb201
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-0udi-0900000000-88938a9c69a2d4daf36a
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-0udi-2900000000-3440f1648bff05d21a31
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-0udi-5900000000-a727755cf1e18764e9d0
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-0udj-9600000000-aa8a18a9ab17508f689d
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-0udj-9200000000-41d7e769a93444ba3751
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0gx0-0940000000-22533c93dd06de52f6a8
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-03di-2090000000-f8dbda8417711177ab80
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-004i-9030000000-cf2c8b3f6a6f68584778
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-03di-0490000000-7be92831389b92fab7f5
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-03fr-7090000000-ae4f1a409501862648a4
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-004i-9500000000-51ba083f137e903d8ade
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-016u-9000000000-62f9e1d42da6e353bfec
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å2)	Source type	Source
[M-H]-	144.6951952	predicted	DarkChem Lite v0.1.0
[M-H]-	144.6683952	predicted	DarkChem Lite v0.1.0
[M-H]-	134.74054	predicted	DeepCCS 1.0 (2019)
[M+H]+	145.1431952	predicted	DarkChem Lite v0.1.0
[M+H]+	145.3481952	predicted	DarkChem Lite v0.1.0
[M+H]+	137.1361	predicted	DeepCCS 1.0 (2019)
[M+Na]+	145.0032952	predicted	DarkChem Lite v0.1.0
[M+Na]+	144.56233	predicted	DeepCCS 1.0 (2019)

Targets

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Details1. Sodium channel protein type 1 subunit alpha

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient (PubMed:14672992). Plays a key role in brain, probably by regulating the moment when neurotransmitters are released in neurons. Involved in sensory perception of mechanical pain: activation in somatosensory neurons induces pain without neurogenic inflammation and produces hypersensitivity to mechanical, but not thermal stimuli

Specific Function

voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential

Gene Name

SCN1A

Uniprot ID

P35498

Uniprot Name

Sodium channel protein type 1 subunit alpha

Molecular Weight

228969.49 Da

References

1. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
2. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
3. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
4. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]

Details2. Sodium channel protein type 2 subunit alpha

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient (PubMed:1325650, PubMed:17021166, PubMed:28256214, PubMed:29844171). Implicated in the regulation of hippocampal replay occurring within sharp wave ripples (SPW-R) important for memory (By similarity)

Specific Function

calmodulin binding

Gene Name

SCN2A

Uniprot ID

Q99250

Uniprot Name

Sodium channel protein type 2 subunit alpha

Molecular Weight

227972.64 Da

References

1. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
4. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]

Details3. Sodium channel protein type 3 subunit alpha

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient (PubMed:24157691, PubMed:28235671, PubMed:29466837). May contribute to the regulation of serotonin/5-hydroxytryptamine release by enterochromaffin cells (By similarity). In pancreatic endocrine cells, required for both glucagon and glucose-induced insulin secretion (By similarity)

Specific Function

voltage-gated sodium channel activity

Gene Name

SCN3A

Uniprot ID

Q9NY46

Uniprot Name

Sodium channel protein type 3 subunit alpha

Molecular Weight

226291.905 Da

References

1. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
4. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]

Details4. Sodium channel protein type 4 subunit alpha

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Pore-forming subunit of a voltage-gated sodium channel complex through which Na(+) ions pass in accordance with their electrochemical gradient. Alternates between resting, activated and inactivated states (PubMed:12766226, PubMed:15318338, PubMed:16890191, PubMed:17898326, PubMed:18690054, PubMed:19347921, PubMed:25707578, PubMed:26700687, PubMed:29992740, PubMed:30190309). Required for normal muscle fiber excitability, normal muscle contraction and relaxation cycles, and constant muscle strength in the presence of fluctuating K(+) levels (PubMed:12766226, PubMed:15318338, PubMed:16890191, PubMed:19347921, PubMed:25707578, PubMed:26659129, PubMed:26700687)

Specific Function

voltage-gated sodium channel activity

Gene Name

SCN4A

Uniprot ID

P35499

Uniprot Name

Sodium channel protein type 4 subunit alpha

Molecular Weight

208059.175 Da

References

1. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
4. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]

Details5. Sodium channel protein type 5 subunit alpha

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient (PubMed:1309946, PubMed:21447824, PubMed:23085483, PubMed:23420830, PubMed:25370050, PubMed:26279430, PubMed:26392562, PubMed:26776555). It is a tetrodotoxin-resistant Na(+) channel isoform (PubMed:1309946). This channel is responsible for the initial upstroke of the action potential. Channel inactivation is regulated by intracellular calcium levels (PubMed:19074138). Required for normal electrical conduction including formation of the infranodal ventricular conduction system and normal action potential configuration, as a result of its interaction with XIRP2 (By similarity)

Specific Function

ankyrin binding

Gene Name

SCN5A

Uniprot ID

Q14524

Uniprot Name

Sodium channel protein type 5 subunit alpha

Molecular Weight

226937.475 Da

References

1. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
4. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]

Details6. Sodium channel protein type 9 subunit alpha

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient (PubMed:15385606, PubMed:16988069, PubMed:17145499, PubMed:17167479, PubMed:19369487, PubMed:24311784, PubMed:25240195, PubMed:26680203, PubMed:7720699). It is a tetrodotoxin-sensitive Na(+) channel isoform (PubMed:7720699). Plays a role in pain mechanisms, especially in the development of inflammatory pain (PubMed:17145499, PubMed:17167479, PubMed:19369487, PubMed:24311784)

Specific Function

voltage-gated sodium channel activity

Gene Name

SCN9A

Uniprot ID

Q15858

Uniprot Name

Sodium channel protein type 9 subunit alpha

Molecular Weight

226370.175 Da

References

1. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
4. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]

Details7. Sodium channel protein type 11 subunit alpha

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Sodium channel mediating the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which sodium ions may pass in accordance with their electrochemical gradient (PubMed:10580103, PubMed:12384689, PubMed:24036948, PubMed:24776970, PubMed:25791876, PubMed:26645915). Involved in membrane depolarization during action potential in nociceptors which function as key relay stations for the electrical transmission of pain signals from the periphery to the central nervous system (PubMed:24036948, PubMed:24776970, PubMed:25791876, PubMed:26645915). Also involved in rapid BDNF-evoked neuronal depolarization (PubMed:12384689)

Specific Function

voltage-gated sodium channel activity

Gene Name

SCN11A

Uniprot ID

Q9UI33

Uniprot Name

Sodium channel protein type 11 subunit alpha

Molecular Weight

204919.66 Da

References

1. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
4. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]

Details8. Sodium channel subunit beta-1

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Regulatory subunit of multiple voltage-gated sodium channel complexes that play important roles in excitable membranes in brain, heart and skeletal muscle. Enhances the presence of the pore-forming alpha subunit at the cell surface and modulates channel gating characteristics and the rate of channel inactivation. Modulates the activity of multiple pore-forming alpha subunits, such as SCN1A, SCN2A, SCN3A, SCN4A, SCN5A and SCN10A

Specific Function

sodium channel inhibitor activity

Gene Name

SCN1B

Uniprot ID

Q07699

Uniprot Name

Sodium channel subunit beta-1

Molecular Weight

24706.955 Da

References

1. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
4. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]

Details9. Sodium channel subunit beta-2

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Crucial in the assembly, expression, and functional modulation of the heterotrimeric complex of the sodium channel. The subunit beta-2 causes an increase in the plasma membrane surface area and in its folding into microvilli. Interacts with TNR may play a crucial role in clustering and regulation of activity of sodium channels at nodes of Ranvier (By similarity)

Specific Function

sodium channel regulator activity

Gene Name

SCN2B

Uniprot ID

O60939

Uniprot Name

Sodium channel subunit beta-2

Molecular Weight

24325.69 Da

References

1. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
4. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]

Details10. Sodium channel regulatory subunit beta-3

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Voltage-gated sodium channels regulatory subunit that modulates channel gating kinetics (PubMed:20558140, PubMed:21051419). Causes unique persistent sodium currents. Inactivates the sodium channel opening more slowly than the subunit beta-1. Its association with NFASC may target the sodium channels to the nodes of Ranvier of developing axons and retain these channels at the nodes in mature myelinated axons (By similarity)

Specific Function

sodium channel inhibitor activity

Gene Name

SCN3B

Uniprot ID

Q9NY72

Uniprot Name

Sodium channel regulatory subunit beta-3

Molecular Weight

24702.08 Da

References

1. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
4. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]

Details11. Sodium channel subunit beta-4

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Modulates channel gating kinetics. Causes negative shifts in the voltage dependence of activation of certain alpha sodium channels, but does not affect the voltage dependence of inactivation. Modulates the susceptibility of the sodium channel to inhibition by toxic peptides from spider, scorpion, wasp and sea anemone venom

Specific Function

sodium channel regulator activity

Gene Name

SCN4B

Uniprot ID

Q8IWT1

Uniprot Name

Sodium channel subunit beta-4

Molecular Weight

24968.755 Da

References

1. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
4. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]

Details12. Voltage-dependent T-type calcium channel subunit alpha-1G

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1G gives rise to T-type calcium currents. T-type calcium channels belong to the 'low-voltage activated (LVA)' group and are strongly blocked by mibefradil. A particularity of this type of channel is an opening at quite negative potentials and a voltage-dependent inactivation. T-type channels serve pacemaking functions in both central neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle. They may also be involved in the modulation of firing patterns of neurons which is important for information processing as well as in cell growth processes.

Specific Function

high voltage-gated calcium channel activity

Gene Name

CACNA1G

Uniprot ID

O43497

Uniprot Name

Voltage-dependent T-type calcium channel subunit alpha-1G

Molecular Weight

262468.62 Da

References

1. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
2. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
3. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
4. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Murata M: Novel therapeutic effects of the anti-convulsant, zonisamide, on Parkinson's disease. Curr Pharm Des. 2004;10(6):687-93. [Article]
8. Murata M: Zonisamide: a new drug for Parkinson's disease. Drugs Today (Barc). 2010 Apr;46(4):251-8. doi: 10.1358/dot.2010.46.4.1490077. [Article]
9. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]
10. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]

Details13. Voltage-dependent T-type calcium channel subunit alpha-1H

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Voltage-sensitive calcium channel that gives rise to T-type calcium currents. T-type calcium channels belong to the 'low-voltage activated (LVA)' group. A particularity of this type of channel is an opening at quite negative potentials, and a voltage-dependent inactivation (PubMed:27149520, PubMed:9670923, PubMed:9930755). T-type channels serve pacemaking functions in both central neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle (Probable). They may also be involved in the modulation of firing patterns of neurons (PubMed:15048902). In the adrenal zona glomerulosa, participates in the signaling pathway leading to aldosterone production in response to either AGT/angiotensin II, or hyperkalemia (PubMed:25907736, PubMed:27729216)

Specific Function

high voltage-gated calcium channel activity

Gene Name

CACNA1H

Uniprot ID

O95180

Uniprot Name

Voltage-dependent T-type calcium channel subunit alpha-1H

Molecular Weight

259160.2 Da

References

1. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
4. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Murata M: Novel therapeutic effects of the anti-convulsant, zonisamide, on Parkinson's disease. Curr Pharm Des. 2004;10(6):687-93. [Article]
8. Murata M: Zonisamide: a new drug for Parkinson's disease. Drugs Today (Barc). 2010 Apr;46(4):251-8. doi: 10.1358/dot.2010.46.4.1490077. [Article]
9. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]
10. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]

Details14. Voltage-dependent T-type calcium channel subunit alpha-1I

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. This channel gives rise to T-type calcium currents. T-type calcium channels belong to the 'low-voltage activated (LVA)' group and are strongly blocked by nickel and mibefradil. A particularity of this type of channels is an opening at quite negative potentials, and a voltage-dependent inactivation. T-type channels serve pacemaking functions in both central neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle. They may also be involved in the modulation of firing patterns of neurons which is important for information processing as well as in cell growth processes. Gates in voltage ranges similar to, but higher than alpha 1G or alpha 1H (By similarity)

Specific Function

high voltage-gated calcium channel activity

Gene Name

CACNA1I

Uniprot ID

Q9P0X4

Uniprot Name

Voltage-dependent T-type calcium channel subunit alpha-1I

Molecular Weight

245100.8 Da

References

1. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. doi: 10.1517/14656560903468728. [Article]
2. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. doi: 10.1517/17425255.4.4.493 . [Article]
3. Sobieszek G, Borowicz KK, Kimber-Trojnar Z, Malek R, Piskorska B, Czuczwar SJ: Zonisamide: a new antiepileptic drug. Pol J Pharmacol. 2003 Sep-Oct;55(5):683-9. [Article]
4. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases]. Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. [Article]
5. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. [Article]
7. Murata M: Novel therapeutic effects of the anti-convulsant, zonisamide, on Parkinson's disease. Curr Pharm Des. 2004;10(6):687-93. [Article]
8. Murata M: Zonisamide: a new drug for Parkinson's disease. Drugs Today (Barc). 2010 Apr;46(4):251-8. doi: 10.1358/dot.2010.46.4.1490077. [Article]
9. Zaccara G, Specchio LM: Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat. 2009;5:249-59. Epub 2009 May 20. [Article]
10. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	56	N/A	N/A	A27521 / A27527 / A27528 / A27529 / A27531 / A4564 / A27532 / A27533 / A27536 / A27537 / A27538 / A27539 / A27541 / A27720 / A27542 / A29210 / A27545 / A27546 / A27547
Ki (nM)	56	7.5	25	A27522
Ki (nM)	56	7.5	22	A27705
Ki (nM)	56	7.5	20	A15775
Ki (nM)	56000	N/A	N/A	A27544
Ki (nM)	14800	N/A	N/A	A27723 / A27724

Details

Binding Properties15. Carbonic anhydrase 1

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Catalyzes the reversible hydration of carbon dioxide (PubMed:10550681, PubMed:16506782, PubMed:16686544, PubMed:16807956, PubMed:17127057, PubMed:17314045, PubMed:17407288, PubMed:18618712, PubMed:19186056, PubMed:19206230). Can hydrate cyanamide to urea (PubMed:10550681)

Specific Function

arylesterase activity

Gene Name

CA1

Uniprot ID

P00915

Uniprot Name

Carbonic anhydrase 1

Molecular Weight

28870.0 Da

References

1. De Simone G, Di Fiore A, Menchise V, Pedone C, Antel J, Casini A, Scozzafava A, Wurl M, Supuran CT: Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies. Bioorg Med Chem Lett. 2005 May 2;15(9):2315-20. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Shank RP, Smith-Swintosky VL, Maryanoff BE: Carbonic anhydrase inhibition. Insight into the characteristics of zonisamide, topiramate, and the sulfamide cognate of topiramate. J Enzyme Inhib Med Chem. 2008 Apr;23(2):271-6. doi: 10.1080/14756360701507001 . [Article]
4. Masuda Y, Karasawa T: Inhibitory effect of zonisamide on human carbonic anhydrase in vitro. Arzneimittelforschung. 1993 Apr;43(4):416-8. [Article]
5. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
6. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
7. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]
8. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Kd (nM)	47.6	N/A	N/A	A27551
Ki (nM)	4300	N/A	N/A	A10349
Ki (nM)	35.2	N/A	N/A	A10942
Ki (nM)	10.3	N/A	N/A	A10942
Ki (nM)	35	N/A	N/A	A27521 / A27527 / A27528 / A27529 / A27531 / A4564 / A27532 / A27554 / A27533 / A27536 / A27537 / A27538 / A27539 / A27541 / A27720 / A27542 / A29210 / A27545 / A27556 / A27546 / A27547
Ki (nM)	35	7.5	25	A27522
Ki (nM)	35	7.5	22	A27705
Ki (nM)	6800	N/A	N/A	A27552
Ki (nM)	35	7.4	25	A29061
Ki (nM)	35	7.5	20	A15775
Ki (nM)	35000	N/A	N/A	A27544
Ki (nM)	1070	N/A	N/A	A27723 / A27724

Details

Binding Properties16. Carbonic anhydrase 2

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Catalyzes the reversible hydration of carbon dioxide (PubMed:11327835, PubMed:11802772, PubMed:11831900, PubMed:12056894, PubMed:12171926, PubMed:1336460, PubMed:14736236, PubMed:15300855, PubMed:15453828, PubMed:15667203, PubMed:15865431, PubMed:16106378, PubMed:16214338, PubMed:16290146, PubMed:16686544, PubMed:16759856, PubMed:16807956, PubMed:17127057, PubMed:17251017, PubMed:17314045, PubMed:17330962, PubMed:17346964, PubMed:17540563, PubMed:17588751, PubMed:17705204, PubMed:18024029, PubMed:18162396, PubMed:18266323, PubMed:18374572, PubMed:18481843, PubMed:18618712, PubMed:18640037, PubMed:18942852, PubMed:1909891, PubMed:1910042, PubMed:19170619, PubMed:19186056, PubMed:19206230, PubMed:19520834, PubMed:19778001, PubMed:7761440, PubMed:7901850, PubMed:8218160, PubMed:8262987, PubMed:8399159, PubMed:8451242, PubMed:8485129, PubMed:8639494, PubMed:9265618, PubMed:9398308). Can also hydrate cyanamide to urea (PubMed:10550681, PubMed:11015219). Stimulates the chloride-bicarbonate exchange activity of SLC26A6 (PubMed:15990874). Essential for bone resorption and osteoclast differentiation (PubMed:15300855). Involved in the regulation of fluid secretion into the anterior chamber of the eye. Contributes to intracellular pH regulation in the duodenal upper villous epithelium during proton-coupled peptide absorption

Specific Function

arylesterase activity

Gene Name

CA2

Uniprot ID

P00918

Uniprot Name

Carbonic anhydrase 2

Molecular Weight

29245.895 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Shank RP, Smith-Swintosky VL, Maryanoff BE: Carbonic anhydrase inhibition. Insight into the characteristics of zonisamide, topiramate, and the sulfamide cognate of topiramate. J Enzyme Inhib Med Chem. 2008 Apr;23(2):271-6. doi: 10.1080/14756360701507001 . [Article]
4. De Simone G, Di Fiore A, Menchise V, Pedone C, Antel J, Casini A, Scozzafava A, Wurl M, Supuran CT: Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies. Bioorg Med Chem Lett. 2005 May 2;15(9):2315-20. [Article]
5. Masuda Y, Karasawa T: Inhibitory effect of zonisamide on human carbonic anhydrase in vitro. Arzneimittelforschung. 1993 Apr;43(4):416-8. [Article]
6. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
7. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
8. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	2200000	N/A	N/A	A20066 / A27533
Ki (nM)	2.20E+06	7.5	20	A15775

Details

Binding Properties17. Carbonic anhydrase 3

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Reversible hydration of carbon dioxide

Specific Function

carbonate dehydratase activity

Gene Name

CA3

Uniprot ID

P07451

Uniprot Name

Carbonic anhydrase 3

Molecular Weight

29557.215 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
5. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]
6. De Simone G, Di Fiore A, Menchise V, Pedone C, Antel J, Casini A, Scozzafava A, Wurl M, Supuran CT: Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies. Bioorg Med Chem Lett. 2005 May 2;15(9):2315-20. [Article]
7. Shank RP, Smith-Swintosky VL, Maryanoff BE: Carbonic anhydrase inhibition. Insight into the characteristics of zonisamide, topiramate, and the sulfamide cognate of topiramate. J Enzyme Inhib Med Chem. 2008 Apr;23(2):271-6. doi: 10.1080/14756360701507001 . [Article]
8. Masuda Y, Karasawa T: Inhibitory effect of zonisamide on human carbonic anhydrase in vitro. Arzneimittelforschung. 1993 Apr;43(4):416-8. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	8590	N/A	N/A	A27528 / A27533
Ki (nM)	8590	7.5	20	A15775
Ki (nM)	38450	N/A	N/A	A27723 / A27724

Details

Binding Properties18. Carbonic anhydrase 4

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Catalyzes the reversible hydration of carbon dioxide into bicarbonate and protons and thus is essential to maintaining intracellular and extracellular pH (PubMed:15563508, PubMed:16686544, PubMed:16807956, PubMed:17127057, PubMed:17314045, PubMed:17652713, PubMed:17705204, PubMed:18618712, PubMed:19186056, PubMed:19206230, PubMed:7625839). May stimulate the sodium/bicarbonate transporter activity of SLC4A4 that acts in pH homeostasis (PubMed:15563508). It is essential for acid overload removal from the retina and retina epithelium, and acid release in the choriocapillaris in the choroid (PubMed:15563508)

Specific Function

carbonate dehydratase activity

Gene Name

CA4

Uniprot ID

P22748

Uniprot Name

Carbonic anhydrase 4

Molecular Weight

35032.075 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
5. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]
6. De Simone G, Di Fiore A, Menchise V, Pedone C, Antel J, Casini A, Scozzafava A, Wurl M, Supuran CT: Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies. Bioorg Med Chem Lett. 2005 May 2;15(9):2315-20. [Article]
7. Shank RP, Smith-Swintosky VL, Maryanoff BE: Carbonic anhydrase inhibition. Insight into the characteristics of zonisamide, topiramate, and the sulfamide cognate of topiramate. J Enzyme Inhib Med Chem. 2008 Apr;23(2):271-6. doi: 10.1080/14756360701507001 . [Article]
8. Masuda Y, Karasawa T: Inhibitory effect of zonisamide on human carbonic anhydrase in vitro. Arzneimittelforschung. 1993 Apr;43(4):416-8. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Kd (nM)	20.6	N/A	N/A	A27551
Ki (nM)	20	N/A	N/A	A27527 / A27533 / A27539
Ki (nM)	20000	N/A	N/A	A27528
Ki (nM)	20	7.5	20	A15775

Details

Binding Properties19. Carbonic anhydrase 5A, mitochondrial

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Mitochondrial carbonic anhydrase that catalyzes the reversible conversion of carbon dioxide to bicarbonate/HCO3 (PubMed:24530203, PubMed:8356065). Mitochondria are impermeable to HCO3, and thus this intramitochondrial carbonic anhydrase is pivotal in providing HCO3 for multiple mitochondrial enzymes that catalyze the formation of essential metabolites of intermediary metabolism in the urea and Krebs cycles (PubMed:24530203)

Specific Function

carbonate dehydratase activity

Gene Name

CA5A

Uniprot ID

P35218

Uniprot Name

Carbonic anhydrase 5A, mitochondrial

Molecular Weight

34750.21 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. De Simone G, Di Fiore A, Menchise V, Pedone C, Antel J, Casini A, Scozzafava A, Wurl M, Supuran CT: Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies. Bioorg Med Chem Lett. 2005 May 2;15(9):2315-20. [Article]
4. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
5. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
6. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	6033	N/A	N/A	A27527 / A27533 / A27539
Ki (nM)	6033000	N/A	N/A	A27528
Ki (nM)	6033	7.5	20	A15775

Details

Binding Properties20. Carbonic anhydrase 5B, mitochondrial

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Mitochondrial carbonic anhydrase that catalyzes the reversible conversion of carbon dioxide to bicarbonate/HCO3

Specific Function

carbonate dehydratase activity

Gene Name

CA5B

Uniprot ID

Q9Y2D0

Uniprot Name

Carbonic anhydrase 5B, mitochondrial

Molecular Weight

36433.43 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. De Simone G, Di Fiore A, Menchise V, Pedone C, Antel J, Casini A, Scozzafava A, Wurl M, Supuran CT: Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies. Bioorg Med Chem Lett. 2005 May 2;15(9):2315-20. [Article]
4. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
5. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
6. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	89	7.5	20	A29212 / A15775
Ki (nM)	89	N/A	N/A	A27533
Ki (nM)	2420	N/A	N/A	A27723 / A27724

Details

Binding Properties21. Carbonic anhydrase 6

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Reversible hydration of carbon dioxide. Its role in saliva is unknown

Specific Function

carbonate dehydratase activity

Gene Name

CA6

Uniprot ID

P23280

Uniprot Name

Carbonic anhydrase 6

Molecular Weight

35366.615 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
5. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	117	N/A	N/A	A27531 / A27533 / A27542 / A27546
Ki (nM)	117	7.4	25	A29061
Ki (nM)	117	7.5	20	A15775

Details

Binding Properties22. Carbonic anhydrase 7

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Reversible hydration of carbon dioxide

Specific Function

carbonate dehydratase activity

Gene Name

CA7

Uniprot ID

P43166

Uniprot Name

Carbonic anhydrase 7

Molecular Weight

29658.235 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
5. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Details23. Carbonic anhydrase-related protein

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Does not have a carbonic anhydrase catalytic activity

Specific Function

carbonate dehydratase activity

Gene Name

CA8

Uniprot ID

P35219

Uniprot Name

Carbonic anhydrase-related protein

Molecular Weight

32972.915 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
5. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	5.1	N/A	N/A	A29003 / A27533 / A29210 / A27546
Ki (nM)	5	7.5	22	A27705
Ki (nM)	5.1	7.5	20	A15775
Ki (nM)	5	N/A	N/A	A27532

Details

Binding Properties24. Carbonic anhydrase 9

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Catalyzes the interconversion between carbon dioxide and water and the dissociated ions of carbonic acid (i.e. bicarbonate and hydrogen ions)

Specific Function

carbonate dehydratase activity

Gene Name

CA9

Uniprot ID

Q16790

Uniprot Name

Carbonic anhydrase 9

Molecular Weight

49697.36 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
5. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Details25. Carbonic anhydrase-related protein 10

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Does not have a catalytic activity

Specific Function

carbonate dehydratase activity

Gene Name

CA10

Uniprot ID

Q9NS85

Uniprot Name

Carbonic anhydrase-related protein 10

Molecular Weight

37562.655 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
5. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Details26. Carbonic anhydrase-related protein 11

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Does not have a catalytic activity

Specific Function

hydro-lyase activity

Gene Name

CA11

Uniprot ID

O75493

Uniprot Name

Carbonic anhydrase-related protein 11

Molecular Weight

36237.885 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
5. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	11000	N/A	N/A	A29003 / A27532 / A27533
Ki (nM)	11000	7.5	20	A15775

Details

Binding Properties27. Carbonic anhydrase 12

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Reversible hydration of carbon dioxide

Specific Function

carbonate dehydratase activity

Gene Name

CA12

Uniprot ID

O43570

Uniprot Name

Carbonic anhydrase 12

Molecular Weight

39450.615 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
5. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	430	N/A	N/A	A27533

Details

Binding Properties28. Carbonic anhydrase 13

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Reversible hydration of carbon dioxide

Specific Function

carbonate dehydratase activity

Gene Name

CA13

Uniprot ID

Q8N1Q1

Uniprot Name

Carbonic anhydrase 13

Molecular Weight

29442.895 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
5. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	5250	N/A	N/A	A29003 / A27533 / A27542 / A29210 / A27546
Ki (nM)	5250	7.5	20	A15775

Details

Binding Properties29. Carbonic anhydrase 14

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Reversible hydration of carbon dioxide

Specific Function

carbonate dehydratase activity

Gene Name

CA14

Uniprot ID

Q9ULX7

Uniprot Name

Carbonic anhydrase 14

Molecular Weight

37667.37 Da

References

1. De Simone G, Scozzafava A, Supuran CT: Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem Biol Drug Des. 2009 Sep;74(3):317-21. doi: 10.1111/j.1747-0285.2009.00857.x. [Article]
2. Supuran CT, Di Fiore A, De Simone G: Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity. Expert Opin Emerg Drugs. 2008 Jun;13(2):383-92. doi: 10.1517/14728214.13.2.383 . [Article]
3. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]
4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. [Article]
5. Authors unspecified: Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	3100	N/A	N/A	A29211

Details

Binding Properties30. Amine oxidase [flavin-containing] B

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Catalyzes the oxidative deamination of primary and some secondary amines such as neurotransmitters, and exogenous amines including the tertiary amine, neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), with concomitant reduction of oxygen to hydrogen peroxide and participates in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (PubMed:11049757, PubMed:11134050, PubMed:20493079, PubMed:8316221, PubMed:8665924). Preferentially degrades benzylamine and phenylethylamine (PubMed:11049757, PubMed:11134050, PubMed:20493079, PubMed:8316221, PubMed:8665924)

Specific Function

aliphatic amine oxidase activity

Gene Name

MAOB

Uniprot ID

P27338

Uniprot Name

Amine oxidase [flavin-containing] B

Molecular Weight

58762.475 Da

References

1. Sonsalla PK, Wong LY, Winnik B, Buckley B: The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34. doi: 10.1016/j.expneurol.2009.11.018. Epub 2009 Dec 4. [Article]
2. Murata M: Novel therapeutic effects of the anti-convulsant, zonisamide, on Parkinson's disease. Curr Pharm Des. 2004;10(6):687-93. [Article]
3. Murata M, Horiuchi E, Kanazawa I: Zonisamide has beneficial effects on Parkinson's disease patients. Neurosci Res. 2001 Dec;41(4):397-9. [Article]
4. Okada M, Kaneko S, Hirano T, Mizuno K, Kondo T, Otani K, Fukushima Y: Effects of zonisamide on dopaminergic system. Epilepsy Res. 1995 Nov;22(3):193-205. [Article]
5. Murata M: Zonisamide: a new drug for Parkinson's disease. Drugs Today (Barc). 2010 Apr;46(4):251-8. doi: 10.1358/dot.2010.46.4.1490077. [Article]
6. Okada M: [Effects of carbamazepine and zonisamide on dopaminergic system in rat striatum and hippocampus]. Nihon Shinkei Seishin Yakurigaku Zasshi. 1994 Oct;14(5):337-54. [Article]
7. Farooq MU, Moore PW, Bhatt A, Aburashed R, Kassab MY: Therapeutic role of zonisamide in neuropsychiatric disorders. Mini Rev Med Chem. 2008 Sep;8(10):968-75. [Article]

Details31. Amine oxidase [flavin-containing] A

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Catalyzes the oxidative deamination of primary and some secondary amine such as neurotransmitters, with concomitant reduction of oxygen to hydrogen peroxide and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (PubMed:18391214, PubMed:20493079, PubMed:24169519, PubMed:8316221). Preferentially oxidizes serotonin (PubMed:20493079, PubMed:24169519). Also catalyzes the oxidative deamination of kynuramine to 3-(2-aminophenyl)-3-oxopropanal that can spontaneously condense to 4-hydroxyquinoline (By similarity)

Specific Function

aliphatic amine oxidase activity

Gene Name

MAOA

Uniprot ID

P21397

Uniprot Name

Amine oxidase [flavin-containing] A

Molecular Weight

59681.27 Da

References

1. Okada M, Kaneko S, Hirano T, Mizuno K, Kondo T, Otani K, Fukushima Y: Effects of zonisamide on dopaminergic system. Epilepsy Res. 1995 Nov;22(3):193-205. [Article]
2. Murata M: Zonisamide: a new drug for Parkinson's disease. Drugs Today (Barc). 2010 Apr;46(4):251-8. doi: 10.1358/dot.2010.46.4.1490077. [Article]

Details32. GABA(A) Receptor Benzodiazepine Binding Site (Protein Group)

Kind

Protein group

Organism

Humans

Pharmacological action

Unknown

Actions

Binder

General Function

Alpha subunit of the heteropentameric ligand-gated chloride channel gated by Gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain (PubMed:23909897, PubMed:25489750, PubMed:29950725, PubMed:30602789). GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interface(s) (PubMed:29950725, PubMed:30602789). When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient (PubMed:23909897, PubMed:29950725, PubMed:30602789). Alpha-1/GABRA1-containing GABAARs are largely synaptic (By similarity). Chloride influx into the postsynaptic neuron following GABAAR opening decreases the neuron ability to generate a new action potential, thereby reducing nerve transmission (By similarity). GABAARs containing alpha-1 and beta-2 or -3 subunits exhibit synaptogenic activity; the gamma-2 subunit being necessary but not sufficient to induce rapid synaptic contacts formation (PubMed:23909897, PubMed:25489750). GABAARs function also as histamine receptor where histamine binds at the interface of two neighboring beta subunits and potentiates GABA response (By similarity). GABAARs containing alpha, beta and epsilon subunits also permit spontaneous chloride channel activity while preserving the structural information required for GABA-gated openings (By similarity). Alpha-1-mediated plasticity in the orbitofrontal cortex regulates context-dependent action selection (By similarity). Together with rho subunits, may also control neuronal and glial GABAergic transmission in the cerebellum (By similarity)

Specific Function

GABA-A receptor activity

---

Components:

Name	UniProt ID
Gamma-aminobutyric acid receptor subunit alpha-1	P14867
Gamma-aminobutyric acid receptor subunit alpha-2	P47869
Gamma-aminobutyric acid receptor subunit alpha-3	P34903
Gamma-aminobutyric acid receptor subunit alpha-5	P31644
Gamma-aminobutyric acid receptor subunit gamma-1	Q8N1C3
Gamma-aminobutyric acid receptor subunit gamma-2	P18507
Gamma-aminobutyric acid receptor subunit gamma-3	Q99928

References

1. Wilfong AA, Willmore LJ: Zonisamide - a review of experience and use in partial seizures. Neuropsychiatr Dis Treat. 2006 Sep;2(3):269-80. doi: 10.2147/nedt.2006.2.3.269. [Article]
2. FDA Approved Drug Products: ZONEGRAN (zonisamide) capsules for oral use [Link]

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Drug created at June 13, 2005 13:24 / Updated at June 02, 2024 21:46