Explore a selection of our essential drug information below, or:
Identification
- Summary
Primidone is an antiepileptic used to treat grand mal, psychomotor, and focal epileptic seizures.
- Brand Names
- Mysoline
- Generic Name
- Primidone
- DrugBank Accession Number
- DB00794
- Background
Primidone is an anticonvulsant used to treat essential tremor as well as grand mal, psychomotor, and focal epileptic seizures.15 Primidone was developed by J Yule Bogue and H C Carrington in 1949.10
Primidone was granted FDA Approval on 8 March 1954.15
- Type
- Small Molecule
- Groups
- Approved, Vet approved
- Structure
Structure for Primidone (DB00794)
- Weight
- Average: 218.2518
Monoisotopic: 218.105527702 - Chemical Formula
- C12H14N2O2
- Synonyms
- 2-deoxyphenobarbital
- 5-Phenyl-5-ethyl-Hexahydropyrimidine-4,6-dione
- Primidon
- Primidona
- Primidone
- Primidonum
- External IDs
- NSC-41701
- Rö 101
Pharmacology
- Indication
Primidone is commonly indicated for the management of grand mal, psychomotor, and focal epileptic seizures.14,15 In addition, it has also been studied and utilized as an effective management of essential tremor.1,2,14
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Essential tremor •••••••••••• ••••••••• •••••• •••••• Management of Focal seizures •••••••••••• Management of Grand mal seizure •••••••••••• Management of Psychomotor seizures •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Primidone alters sodium and calcium channel transport, reducing the frequency of nerve firing, which may be responsible for its effect on convulsions and essential tremor.4 Primidone has a wide therapeutic window as doses of 50-1000mg/day were effective.4 Patients should be counselled regarding the risk of status epilepticus with abrupt cessation of primidone.15
- Mechanism of action
Primidone and its metabolites, phenobarbital and phenylethylmalonamide (PEMA), are active anticonvulsants.4 Primidone does not directly interact with GABA-A receptors or chloride channels but phenobarbital does.4 Primidone alters transmembrane sodium and calcium channel transport, reducing the frequency of nerve firing, which may be responsible for the primidone’s effect on convulsions and essential tremor.4
Target Actions Organism AGamma-aminobutyric acid receptor subunit alpha-2 potentiatorHumans AGamma-aminobutyric acid receptor subunit alpha-3 potentiatorHumans AGamma-aminobutyric acid receptor subunit alpha-4 potentiatorHumans AGamma-aminobutyric acid receptor subunit alpha-5 potentiatorHumans AGamma-aminobutyric acid receptor subunit alpha-6 potentiatorHumans AGABA(A) Receptor positive allosteric modulatorHumans AGamma-aminobutyric acid receptor subunit alpha-1 potentiatorHumans UNeuronal acetylcholine receptor subunit alpha-4 antagonistHumans UNeuronal acetylcholine receptor subunit alpha-7 antagonistHumans UGlutamate receptor 2 antagonistHumans UGlutamate receptor ionotropic, kainate 2 antagonistHumans - Absorption
Oral primidone is up to 80% bioavailable with a Tmax if 2-4h.4,6 A 500mg oral dose of primidone Reaches a Cmax of 2.7±0.4µg/mL with a Tmax of 0.5-7h.7 Data regarding the AUC of primidone is not readily available.15
- Volume of distribution
- Protein binding
Primidone is 10.78-13.70% protein bound in serum.3
- Metabolism
Primidone is metabolized to phenobarbitol and phenylethylmalonamide (PEMA).11 This metabolism is largely mediated by CYP2C9,12,4,5 CYP2C19,13,12,5 and CYP2E1.12,5
Hover over products below to view reaction partners
- Route of elimination
Primidone is 72.9-80.6% recovered in urine.8
- Half-life
The half life of primidone is 7-22h in adults, 5-11h in children, and 8-80h in newborns.6
- Clearance
Primidone is cleared at a rate of 30mL/min.7
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
The oral LD50 in rats is 1500mg/kg and in mice is 280mg/kg.16 The intraperitoneal LD50 in rats was 240mg/kg and in mice was 332mg/kg.16
Patients experiencing a primidone overdose may present with CNS depression, coma, respiratory depression, suppressed reflexes, suppressed response to pain, hypotension, and decreased urine output.9 Overdose should be treated with symptomatic and supportive treatment, including the removal of unabsorbed drug.9
- 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.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be increased when combined with Primidone. Abacavir The metabolism of Abacavir can be increased when combined with Primidone. Abaloparatide Primidone may increase the hypotensive activities of Abaloparatide. Abatacept The metabolism of Primidone can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Primidone. - Food Interactions
- Avoid alcohol.
- Avoid St. John's Wort.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Images
- International/Other Brands
- Liskantin (Desitin) / Mizodin (Unia) / Mylepsinum / Pridona (Psicofarma) / Primid (Apsen) / Prysoline (Rekah) / Sertan (Alkaloida)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Mysoline Tablet 250 mg/1 Oral Bausch Health US, LLC 2009-06-24 Not applicable US 
Mysoline Tablet 50 mg/1 Oral Bausch Health US, LLC 2009-06-24 Not applicable US Mysoline 250mg Tab Tablet 250 mg Oral Elan Pharmaceuticals 1994-12-31 2004-08-05 Canada 
Mysoline Pediatric Chewable Tablets 125mg Tablet 125 mg Oral Elan Pharmaceuticals 1994-12-31 2004-08-05 Canada Mysoline Tab 125mg Tablet 125 mg / tab Oral Ayerst Laboratories 1963-12-31 1996-09-10 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Primidone Tablet 250 mg/1 Oral Lannett Company, Inc. 1978-12-01 Not applicable US Primidone Tablet 250 mg/1 Oral Ncs Health Care Of Ky, Inc Dba Vangard Labs 2006-07-01 Not applicable US Primidone Tablet 50 mg/1 Oral Impax Generics 2008-02-12 2014-02-28 US Primidone Tablet 50 mg/1 Oral Advagen Pharma Limited 2022-06-28 Not applicable US Primidone Tablet 50 mg/1 Oral Oceanside Pharmaceuticals 2018-05-21 Not applicable US
Categories
- ATC Codes
- N05CB01 — Combinations of barbiturates
- N05CB — Barbiturates, combinations
- N05C — HYPNOTICS AND SEDATIVES
- N05 — PSYCHOLEPTICS
- N — NERVOUS SYSTEM
- Drug Categories
- Anti-epileptic Agent
- Anticholinergic Agents
- Anticonvulsants
- Barbiturates
- Barbiturates and Derivatives
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP1A2 Inducers
- Cytochrome P-450 CYP1A2 Inducers (strength unknown)
- Cytochrome P-450 CYP1A2 Inducers (strong)
- Cytochrome P-450 CYP2C19 Inducers
- Cytochrome P-450 CYP2C19 Inducers (strength unknown)
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inducers (strength unknown)
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2E1 Inducers
- Cytochrome P-450 CYP2E1 Inducers (strength unknown)
- Cytochrome P-450 CYP2E1 Substrates
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Inducers (strong)
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Inducers (strong)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Decreased Central Nervous System Disorganized Electrical Activity
- Enzyme Inducing Antiepileptic Drugs
- GABA Agents
- GABA Modulators
- Hypnotics and Sedatives
- Nervous System
- Neurotransmitter Agents
- Nicotinic Antagonists
- Phenobarbital and similars
- Psycholeptics
- Pyrimidines
- Pyrimidinones
- UGT1A1 Inducers
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as hydropyrimidines. These are compounds containing a hydrogenated pyrimidine ring (i.e. containing less than the maximum number of double bonds.).
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Diazines
- Sub Class
- Pyrimidines and pyrimidine derivatives
- Direct Parent
- Hydropyrimidines
- Alternative Parents
- Benzene and substituted derivatives / Cyclic carboximidic acids / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Organopnictogen compounds / Organooxygen compounds / Organonitrogen compounds / Hydrocarbon derivatives
- Substituents
- 2,5-dihydropyrimidine / Aromatic heteromonocyclic compound / Azacycle / Benzenoid / Cyclic carboximidic acid / Hydrocarbon derivative / Hydropyrimidine / Monocyclic benzene moiety / Organic 1,3-dipolar compound / Organic nitrogen compound
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- pyrimidone (CHEBI:8412)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 13AFD7670Q
- CAS number
- 125-33-7
- InChI Key
- DQMZLTXERSFNPB-UHFFFAOYSA-N
- InChI
- InChI=1S/C12H14N2O2/c1-2-12(9-6-4-3-5-7-9)10(15)13-8-14-11(12)16/h3-7H,2,8H2,1H3,(H,13,15)(H,14,16)
- IUPAC Name
- 5-ethyl-5-phenyl-1,3-diazinane-4,6-dione
- SMILES
- CCC1(C(=O)NCNC1=O)C1=CC=CC=C1
References
- General References
- Rajput AH, Rajput A: Medical treatment of essential tremor. J Cent Nerv Syst Dis. 2014 Apr 21;6:29-39. doi: 10.4137/JCNSD.S13570. eCollection 2014. [Article]
- Schneider SA, Deuschl G: The treatment of tremor. Neurotherapeutics. 2014 Jan;11(1):128-38. doi: 10.1007/s13311-013-0230-5. [Article]
- Haidukewych D, Rodin EA: Serial free and plasma valproic acid and phenytoin monitoring and drug interactions. Ther Drug Monit. 1981;3(3):303-7. doi: 10.1097/00007691-198103000-00013. [Article]
- Hedera P, Cibulcik F, Davis TL: Pharmacotherapy of essential tremor. J Cent Nerv Syst Dis. 2013 Dec 22;5:43-55. doi: 10.4137/JCNSD.S6561. [Article]
- Marvanova M: Pharmacokinetic characteristics of antiepileptic drugs (AEDs). Ment Health Clin. 2016 Mar 8;6(1):8-20. doi: 10.9740/mhc.2015.01.008. eCollection 2016 Jan. [Article]
- Patsalos PN, Spencer EP, Berry DJ: Therapeutic Drug Monitoring of Antiepileptic Drugs in Epilepsy: A 2018 Update. Ther Drug Monit. 2018 Oct;40(5):526-548. doi: 10.1097/FTD.0000000000000546. [Article]
- Lee CS, Marbury TC, Perchalski RT, Wilder BJ: Pharmacokinetics of primidone elimination by uremic patients. J Clin Pharmacol. 1982 Jul;22(7):301-8. doi: 10.1002/j.1552-4604.1982.tb02679.x. [Article]
- Treston AM, Hooper WD: Urinary metabolites of phenobarbitone, primidone, and their N-methyl and N-ethyl derivatives in humans. Xenobiotica. 1992 Apr;22(4):385-94. doi: 10.3109/00498259209046650. [Article]
- van Heijst AN, de Jong W, Seldenrijk R, van Dijk A: Coma and crystalluria: a massive primidone intoxication treated with haemoperfusion. J Toxicol Clin Toxicol. 1983 Jun;20(4):307-18. doi: 10.3109/15563658308990598. [Article]
- HANDLEY R, STEWART AS: Mysoline; a new drug in the treatment of epilepsy. Lancet. 1952 Apr 12;1(6711):742-4. doi: 10.1016/s0140-6736(52)90500-x. [Article]
- El-Masri HA, Portier CJ: Physiologically based pharmacokinetics model of primidone and its metabolites phenobarbital and phenylethylmalonamide in humans, rats, and mice. Drug Metab Dispos. 1998 Jun;26(6):585-94. [Article]
- Zaccara G, Perucca E: Interactions between antiepileptic drugs, and between antiepileptic drugs and other drugs. Epileptic Disord. 2014 Dec;16(4):409-31. doi: 10.1684/epd.2014.0714. [Article]
- Tanaka E: Clinically significant pharmacokinetic drug interactions between antiepileptic drugs. J Clin Pharm Ther. 1999 Apr;24(2):87-92. doi: 10.1046/j.1365-2710.1999.00201.x. [Article]
- Electronic Medicines Compendium: Primidone 50 mg Tablet Monograph [Link]
- FDA Approved Drug Products: Mysoline Primidone Oral Tablets [Link]
- Cayman Chemical: Primidone MSDS [Link]
- External Links
- Human Metabolome Database
- HMDB0014932
- KEGG Drug
- D00474
- KEGG Compound
- C07371
- PubChem Compound
- 4909
- PubChem Substance
- 46507775
- ChemSpider
- 4740
- BindingDB
- 50248152
- 8691
- ChEBI
- 8412
- ChEMBL
- CHEMBL856
- ZINC
- ZINC000000001979
- Therapeutic Targets Database
- DAP000678
- PharmGKB
- PA451105
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Primidone
- FDA label
- Download (108 KB)
- MSDS
- Download (65.5 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data2 Withdrawn Treatment Clopidogrel Resistance / Secondary Stroke Prevention 1 somestatus stop reason just information to hide 1 Completed Basic Science Therapeutic Equivalency 1 somestatus stop reason just information to hide 1 Completed Treatment Healthy Volunteers (HV) 1 somestatus stop reason just information to hide Not Available Completed Not Available Epilepsy 1 somestatus stop reason just information to hide Not Available Completed Not Available Essential Tremor 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Xcel pharmaceuticals
- Valeant pharmaceuticals international
- Amneal pharmaceutical
- Dr reddys laboratories ltd
- Impax laboratories inc
- Lannett co inc
- Mutual pharmaceutical co inc
- Vintage pharmaceuticals inc
- Watson laboratories inc
- West ward pharmaceutical corp
- Packagers
- Amerisource Health Services Corp.
- Amneal Pharmaceuticals
- Astellas Pharma Inc.
- Atlantic Biologicals Corporation
- Avkare Incorporated
- Cardinal Health
- Comprehensive Consultant Services Inc.
- Doctor Reddys Laboratories Ltd.
- Global Pharmaceuticals
- Heartland Repack Services LLC
- Impax Laboratories Inc.
- Kaiser Foundation Hospital
- Lake Erie Medical and Surgical Supply
- Lannett Co. Inc.
- Major Pharmaceuticals
- Murfreesboro Pharmaceutical Nursing Supply
- Mutual Pharmaceutical Co.
- Patheon Inc.
- PCA LLC
- Pharmaceutical Packaging Center
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmacy Service Center
- Physicians Total Care Inc.
- Prepak Systems Inc.
- Professional Co.
- Qualitest
- Remedy Repack
- Resource Optimization and Innovation LLC
- Richmond Pharmacy
- Valeant Ltd.
- Vangard Labs Inc.
- Vintage Pharmaceuticals Inc.
- Watson Pharmaceuticals
- West-Ward Pharmaceuticals
- Dosage Forms
Form Route Strength Suspension Oral 125 mg Tablet Oral 0.25 G Tablet Oral 250 mg Tablet Oral 250.000 mg Tablet Oral 125 mg Tablet Oral 125 mg/1 Tablet Oral 250 mg/1 Tablet Oral 50 mg/1 Tablet Oral 125 mg / tab Tablet Oral 250 mg / tab Tablet Oral - Prices
Unit description Cost Unit Primidone powder 10.56USD g Mysoline 250 mg tablet 6.52USD tablet Mysoline 50 mg tablet 1.26USD tablet Primidone 250 mg tablet 1.02USD tablet Primidone 50 mg tablet 0.51USD tablet Apo-Primidone 250 mg Tablet 0.09USD tablet Apo-Primidone 125 mg Tablet 0.06USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 281.5 °C PhysProp water solubility 500 mg/L (at 22 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992) logP 0.91 HANSCH,C ET AL. (1995) logS -2.64 ADME Research, USCD - Predicted Properties
Property Value Source Water Solubility 1.04 mg/mL ALOGPS logP 0.62 ALOGPS logP 1.12 Chemaxon logS -2.3 ALOGPS pKa (Strongest Acidic) 11.5 Chemaxon pKa (Strongest Basic) -6.2 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 58.2 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 59.04 m3·mol-1 Chemaxon Polarizability 22.44 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 + 0.9907 Blood Brain Barrier + 0.9642 Caco-2 permeable - 0.5593 P-glycoprotein substrate Substrate 0.5222 P-glycoprotein inhibitor I Non-inhibitor 0.536 P-glycoprotein inhibitor II Non-inhibitor 0.9048 Renal organic cation transporter Non-inhibitor 0.8298 CYP450 2C9 substrate Non-substrate 0.7961 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Non-substrate 0.6863 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Non-inhibitor 0.924 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8682 Ames test AMES toxic 0.9107 Carcinogenicity Non-carcinogens 0.7814 Biodegradation Not ready biodegradable 0.982 Rat acute toxicity 2.1941 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9912 hERG inhibition (predictor II) Non-inhibitor 0.8735
Spectra
- Mass Spec (NIST)
- Download (9.01 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 152.5808268 predictedDarkChem Lite v0.1.0 [M-H]- 152.6351268 predictedDarkChem Lite v0.1.0 [M-H]- 152.5837268 predictedDarkChem Lite v0.1.0 [M-H]- 151.50157 predictedDeepCCS 1.0 (2019) [M+H]+ 153.7144268 predictedDarkChem Lite v0.1.0 [M+H]+ 153.5146268 predictedDarkChem Lite v0.1.0 [M+H]+ 153.6865268 predictedDarkChem Lite v0.1.0 [M+H]+ 153.85959 predictedDeepCCS 1.0 (2019) [M+Na]+ 153.0126268 predictedDarkChem Lite v0.1.0 [M+Na]+ 162.9773134 predictedDarkChem Lite v0.1.0 [M+Na]+ 159.95273 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- 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:10449790, PubMed:29961870, PubMed:31032849). 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 interfaces (By similarity). When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient (PubMed:10449790). 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). The alpha-2 subunit exhibits synaptogenic activity together with beta-2 and very little to no activity together with beta-3, the gamma-2 subunit being necessary but not sufficient to induce rapid synaptic contacts formation (By similarity)
- Specific Function
- Benzodiazepine receptor activity
- Gene Name
- GABRA2
- Uniprot ID
- P47869
- Uniprot Name
- Gamma-aminobutyric acid receptor subunit alpha-2
- Molecular Weight
- 51325.85 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- 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:16412217, PubMed:29053855). 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) (By similarity). When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient (PubMed:16412217, PubMed:29053855). Chloride influx into the postsynaptic neuron following GABAAR opening decreases the neuron ability to generate a new action potential, thereby reducing nerve transmission (PubMed:16412217, PubMed:29053855)
- Specific Function
- Benzodiazepine receptor activity
- Gene Name
- GABRA3
- Uniprot ID
- P34903
- Uniprot Name
- Gamma-aminobutyric acid receptor subunit alpha-3
- Molecular Weight
- 55164.055 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- 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:35355020). 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:35355020). When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient (PubMed:35355020). GABAARs containing alpha-4 are predominantly extrasynaptic, contributing to tonic inhibition in dentate granule cells and thalamic relay neurons (By similarity). Extrasynaptic alpha-4-containing GABAARs control levels of excitability and network activity (By similarity). GABAAR containing alpha-4-beta-3-delta subunits can simultaneously bind GABA and histamine where histamine binds at the interface of two neighboring beta subunits, which may be involved in the regulation of sleep and wakefulness (PubMed:35355020)
- Specific Function
- Benzodiazepine receptor activity
- Gene Name
- GABRA4
- Uniprot ID
- P48169
- Uniprot Name
- Gamma-aminobutyric acid receptor subunit alpha-4
- Molecular Weight
- 61622.645 Da
References
- Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- 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:14993607, PubMed:29961870, PubMed:30140029, PubMed:31056671). 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:30140029). When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient (PubMed:14993607, PubMed:30140029). GABAARs containing alpha-5/GABRA5 subunits are mainly extrasynaptic and contribute to the tonic GABAergic inhibition in the hippocampus (By similarity). Extrasynaptic alpha-5-containing GABAARs in CA1 pyramidal neurons play a role in learning and memory processes (By similarity)
- Specific Function
- Gaba receptor binding
- Gene Name
- GABRA5
- Uniprot ID
- P31644
- Uniprot Name
- Gamma-aminobutyric acid receptor subunit alpha-5
- Molecular Weight
- 52145.645 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- 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:8632757). 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) (By similarity). When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient (By similarity). Alpha-6/GABRA6 subunits are found at both synaptic and extrasynaptic sites (PubMed:8632757). 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). Extrasynaptic alpha-6-containing receptors contribute to the tonic GABAergic inhibition. Alpha-6 subunits are also present on glutamatergic synapses (By similarity)
- Specific Function
- Benzodiazepine receptor activity
- Gene Name
- GABRA6
- Uniprot ID
- Q16445
- Uniprot Name
- Gamma-aminobutyric acid receptor subunit alpha-6
- Molecular Weight
- 51023.69 Da
References
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Positive allosteric modulator
- Curator comments
- This activity is performed by phenobarbital, a metabolite of primidone.
- 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:
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- 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
- Gene Name
- GABRA1
- Uniprot ID
- P14867
- Uniprot Name
- Gamma-aminobutyric acid receptor subunit alpha-1
- Molecular Weight
- 51801.395 Da
References
- Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57. [Article]
- Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [Article]
- Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [Article]
- Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeable to sodium ions
- Specific Function
- Acetylcholine binding
- Gene Name
- CHRNA4
- Uniprot ID
- P43681
- Uniprot Name
- Neuronal acetylcholine receptor subunit alpha-4
- Molecular Weight
- 69956.47 Da
References
- Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [Article]
- Arias HR, Bhumireddy P: Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors. Curr Protein Pept Sci. 2005 Oct;6(5):451-72. [Article]
- Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is blocked by alpha-bungarotoxin
- Specific Function
- Acetylcholine binding
- Gene Name
- CHRNA7
- Uniprot ID
- P36544
- Uniprot Name
- Neuronal acetylcholine receptor subunit alpha-7
- Molecular Weight
- 56448.925 Da
References
- Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [Article]
- Arias HR, Bhumireddy P: Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors. Curr Protein Pept Sci. 2005 Oct;6(5):451-72. [Article]
- Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Ionotropic glutamate receptor that functions as a ligand-gated cation channel, gated by L-glutamate and glutamatergic agonists such as alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), quisqualic acid, and kainic acid (PubMed:20614889, PubMed:31300657, PubMed:8003671). L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system and plays an important role in fast excitatory synaptic transmission (PubMed:14687553). Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse upon entry of monovalent and divalent cations such as sodium and calcium (PubMed:20614889, PubMed:8003671). The receptor then desensitizes rapidly and enters in a transient inactive state, characterized by the presence of bound agonist (By similarity). In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of L-glutamate (By similarity). Through complex formation with NSG1, GRIP1 and STX12 controls the intracellular fate of AMPAR and the endosomal sorting of the GRIA2 subunit toward recycling and membrane targeting (By similarity)
- Specific Function
- Ampa glutamate receptor activity
- Gene Name
- GRIA2
- Uniprot ID
- P42262
- Uniprot Name
- Glutamate receptor 2
- Molecular Weight
- 98820.32 Da
References
- Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [Article]
- Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Ionotropic glutamate receptor that functions as a cation permeable ligand-gated ion channel, gated by L-glutamate and the glutamatergic agonist kainic acid. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist (PubMed:14511640, PubMed:28180184, PubMed:34375587, PubMed:7536611, PubMed:8730589). Modulates cell surface expression of NETO2. In association with GRIK3, involved in presynaptic facilitation of glutamate release at hippocampal mossy fiber synapses (By similarity)
- Specific Function
- Extracellularly glutamate-gated ion channel activity
- Gene Name
- GRIK2
- Uniprot ID
- Q13002
- Uniprot Name
- Glutamate receptor ionotropic, kainate 2
- Molecular Weight
- 102582.475 Da
References
- Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [Article]
- Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids and steroids (PubMed:12865317, PubMed:15766564, PubMed:19965576, PubMed:21576599, PubMed:7574697, PubMed:9435160, PubMed:9866708). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:12865317, PubMed:15766564, PubMed:19965576, PubMed:21576599, PubMed:7574697, PubMed:9435160, PubMed:9866708). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:15766564, PubMed:19965576, PubMed:7574697, PubMed:9866708). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Exhibits low catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes bisallylic hydroxylation and hydroxylation with double-bond migration of polyunsaturated fatty acids (PUFA) (PubMed:9435160, PubMed:9866708). Also metabolizes plant monoterpenes such as limonene. Oxygenates (R)- and (S)-limonene to produce carveol and perillyl alcohol (PubMed:11950794). Contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenytoin, tolbutamide and losartan (PubMed:25994031)
- Specific Function
- (r)-limonene 6-monooxygenase activity
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Zaccara G, Perucca E: Interactions between antiepileptic drugs, and between antiepileptic drugs and other drugs. Epileptic Disord. 2014 Dec;16(4):409-31. doi: 10.1684/epd.2014.0714. [Article]
- Hedera P, Cibulcik F, Davis TL: Pharmacotherapy of essential tremor. J Cent Nerv Syst Dis. 2013 Dec 22;5:43-55. doi: 10.4137/JCNSD.S6561. [Article]
- Marvanova M: Pharmacokinetic characteristics of antiepileptic drugs (AEDs). Ment Health Clin. 2016 Mar 8;6(1):8-20. doi: 10.9740/mhc.2015.01.008. eCollection 2016 Jan. [Article]
- primidone - Drug Summary [Link]
- MONOGRAPH, Primidone [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- Curator comments
- As the major active metabolite of primidone is phenobarbital, this drug is an inducer of CYP2C19.
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of polyunsaturated fatty acids (PUFA) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Catalyzes the hydroxylation of carbon-hydrogen bonds. Hydroxylates PUFA specifically at the omega-1 position (PubMed:18577768). Catalyzes the epoxidation of double bonds of PUFA (PubMed:19965576, PubMed:20972997). Also metabolizes plant monoterpenes such as limonene. Oxygenates (R)- and (S)-limonene to produce carveol and perillyl alcohol (PubMed:11950794). Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine. Hydroxylates fenbendazole at the 4' position (PubMed:23959307)
- Specific Function
- (r)-limonene 6-monooxygenase activity
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55944.565 Da
References
- Tanaka E: Clinically significant pharmacokinetic drug interactions between antiepileptic drugs. J Clin Pharm Ther. 1999 Apr;24(2):87-92. doi: 10.1046/j.1365-2710.1999.00201.x. [Article]
- Zaccara G, Perucca E: Interactions between antiepileptic drugs, and between antiepileptic drugs and other drugs. Epileptic Disord. 2014 Dec;16(4):409-31. doi: 10.1684/epd.2014.0714. [Article]
- Marvanova M: Pharmacokinetic characteristics of antiepileptic drugs (AEDs). Ment Health Clin. 2016 Mar 8;6(1):8-20. doi: 10.9740/mhc.2015.01.008. eCollection 2016 Jan. [Article]
- Primidine Prescribing Information, Canada [File]
- Primidone FDA label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of fatty acids (PubMed:10553002, PubMed:18577768). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10553002, PubMed:18577768). Catalyzes the hydroxylation of carbon-hydrogen bonds. Hydroxylates fatty acids specifically at the omega-1 position displaying the highest catalytic activity for saturated fatty acids (PubMed:10553002, PubMed:18577768). May be involved in the oxidative metabolism of xenobiotics (Probable)
- Specific Function
- 4-nitrophenol 2-monooxygenase activity
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- Molecular Weight
- 56848.42 Da
References
- Zaccara G, Perucca E: Interactions between antiepileptic drugs, and between antiepileptic drugs and other drugs. Epileptic Disord. 2014 Dec;16(4):409-31. doi: 10.1684/epd.2014.0714. [Article]
- Marvanova M: Pharmacokinetic characteristics of antiepileptic drugs (AEDs). Ment Health Clin. 2016 Mar 8;6(1):8-20. doi: 10.9740/mhc.2015.01.008. eCollection 2016 Jan. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
- Specific Function
- 1,8-cineole 2-exo-monooxygenase activity
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Spina E, Pisani F, Perucca E: Clinically significant pharmacokinetic drug interactions with carbamazepine. An update. Clin Pharmacokinet. 1996 Sep;31(3):198-214. doi: 10.2165/00003088-199631030-00004. [Article]
- Benit CP, Vecht CJ: Seizures and cancer: drug interactions of anticonvulsants with chemotherapeutic agents, tyrosine kinase inhibitors and glucocorticoids. Neurooncol Pract. 2016 Dec;3(4):245-260. doi: 10.1093/nop/npv038. Epub 2015 Oct 11. [Article]
- Tanaka E: Clinically significant pharmacokinetic drug interactions between antiepileptic drugs. J Clin Pharm Ther. 1999 Apr;24(2):87-92. doi: 10.1046/j.1365-2710.1999.00201.x. [Article]
- Hedera P, Cibulcik F, Davis TL: Pharmacotherapy of essential tremor. J Cent Nerv Syst Dis. 2013 Dec 22;5:43-55. doi: 10.4137/JCNSD.S6561. [Article]
- Marvanova M: Pharmacokinetic characteristics of antiepileptic drugs (AEDs). Ment Health Clin. 2016 Mar 8;6(1):8-20. doi: 10.9740/mhc.2015.01.008. eCollection 2016 Jan. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:11555828, PubMed:12865317). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2 (PubMed:11555828, PubMed:12865317). Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). May act as a major enzyme for all-trans retinoic acid biosynthesis in the liver. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid (PubMed:10681376). Primarily catalyzes stereoselective epoxidation of the last double bond of polyunsaturated fatty acids (PUFA), displaying a strong preference for the (R,S) stereoisomer (PubMed:19965576). Catalyzes bisallylic hydroxylation and omega-1 hydroxylation of PUFA (PubMed:9435160). May also participate in eicosanoids metabolism by converting hydroperoxide species into oxo metabolites (lipoxygenase-like reaction, NADPH-independent) (PubMed:21068195). Plays a role in the oxidative metabolism of xenobiotics. Catalyzes the N-hydroxylation of heterocyclic amines and the O-deethylation of phenacetin (PubMed:14725854). Metabolizes caffeine via N3-demethylation (Probable)
- Specific Function
- Aromatase activity
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58406.915 Da
References
- Johannessen SI, Landmark CJ: Antiepileptic drug interactions - principles and clinical implications. Curr Neuropharmacol. 2010 Sep;8(3):254-67. doi: 10.2174/157015910792246254. [Article]
- Hedera P, Cibulcik F, Davis TL: Pharmacotherapy of essential tremor. J Cent Nerv Syst Dis. 2013 Dec 22;5:43-55. doi: 10.4137/JCNSD.S6561. [Article]
- Marvanova M: Pharmacokinetic characteristics of antiepileptic drugs (AEDs). Ment Health Clin. 2016 Mar 8;6(1):8-20. doi: 10.9740/mhc.2015.01.008. eCollection 2016 Jan. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 3 lacks transferase activity but acts as a negative regulator of isoform 1 (By similarity)
- Specific Function
- Enzyme binding
Components:
References
- Johannessen SI, Landmark CJ: Antiepileptic drug interactions - principles and clinical implications. Curr Neuropharmacol. 2010 Sep;8(3):254-67. doi: 10.2174/157015910792246254. [Article]
- Marvanova M: Pharmacokinetic characteristics of antiepileptic drugs (AEDs). Ment Health Clin. 2016 Mar 8;6(1):8-20. doi: 10.9740/mhc.2015.01.008. eCollection 2016 Jan. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Calcium channel mediating constitutive calcium ion entry. Its activity is increased by reduction in extracellular osmolarity, by store depletion and muscarinic receptor activation. In addition, forms heteromultimeric ion channels with TRPM1 which are permeable for calcium and zinc ions (PubMed:21278253)
- Specific Function
- Calcium channel activity
- Gene Name
- TRPM3
- Uniprot ID
- Q9HCF6
- Uniprot Name
- Transient receptor potential cation channel subfamily M member 3
- Molecular Weight
- 197569.225 Da
References
- Krugel U, Straub I, Beckmann H, Schaefer M: Primidone inhibits TRPM3 and attenuates thermal nociception in vivo. Pain. 2017 May;158(5):856-867. doi: 10.1097/j.pain.0000000000000846. [Article]
Drug created at June 13, 2005 13:24 / Updated at September 07, 2024 14:25