Identification
- Summary
Brinzolamide is a carbonic anhydrase inhibitor used for the reduction of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
- Brand Names
- Azarga, Azopt, Simbrinza
- Generic Name
- Brinzolamide
- DrugBank Accession Number
- DB01194
- Background
Brinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase inhibitor. Carbonic anhydrase (CA) is an enzyme found in many tissues of the body including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II (CA-II). Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in intraocular pressure. Brinzolamide is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Brinzolamide (DB01194)
- Weight
- Average: 383.507
Monoisotopic: 383.064332867 - Chemical Formula
- C12H21N3O5S3
- Synonyms
- Brinzolamida
- Brinzolamide
- External IDs
- AL-4862
Pharmacology
- Indication
For the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Used in the treatment of glaucoma, brinzolamide inhibits aqueous humor formation and reduces elevated intraocular pressure. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss. Brinzolamide can decrease intraocular pressure by approximately 16-19% in patients with elevated intraocular pressure.
- Mechanism of action
Brinzolamide is a highly specific inhibitor of CA-II, which is the main CA isoenzyme involved in the secretion of aqueous humor. Inhibition of CA in the ciliary process of the eye slows the formation of bicarbonate, and reduces sodium and fluid transport. This results in a reduction in the rate of aqueous humor secretion and the intraocular pressure. Brinzolamide is absorbed systemically following topical ocular administration. Since it has a high affinity for CA-II, brinzolamide binds extensively to red blood cells, where CA-II is primarily found. As sufficient CA-II activity remains, adverse effects resulting from the systemic inhibition of CA by brinzolamide are not observed. The metabolite N-desethyl brinzolamide is also formed. This metabolite binds to CA and accumulates in red blood cells as well. In the presence of brinzolamide, the metabolite binds mainly to carbonic anhydrase I (CA-I).
Target Actions Organism ACarbonic anhydrase 2 inhibitorHumans UCarbonic anhydrase 1 inhibitorHumans UCarbonic anhydrase 4 inhibitorHumans UCarbonic anhydrase 5A, mitochondrial inhibitorHumans UCarbonic anhydrase 3 inhibitorHumans - Absorption
Absorbed into systemic circulation following topical ocular application
- Volume of distribution
Not Available
- Protein binding
Approximately 60%.
- Metabolism
Ophthalmic
- Route of elimination
Not Available
- Half-life
111 days
- Clearance
Not Available
- Adverse Effects
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Not Available
- 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 softwareAbametapir The serum concentration of Brinzolamide can be increased when it is combined with Abametapir. Benzylpenicillin Brinzolamide may decrease the excretion rate of Benzylpenicillin which could result in a higher serum level. Cenobamate The serum concentration of Brinzolamide can be decreased when it is combined with Cenobamate. Empagliflozin Empagliflozin may increase the diuretic activities of Brinzolamide. Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Brinzolamide. Magnesium The serum concentration of Magnesium can be decreased when it is combined with Brinzolamide. Meloxicam The therapeutic efficacy of Brinzolamide can be decreased when used in combination with Meloxicam. Oliceridine The therapeutic efficacy of Brinzolamide can be decreased when used in combination with Oliceridine. Ritonavir The serum concentration of Brinzolamide can be increased when it is combined with Ritonavir. Satralizumab The serum concentration of Brinzolamide can be decreased when it is combined with Satralizumab. 
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- No interactions found.
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.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Azopt Suspension / drops 10 mg/ml Ophthalmic Novartis Europharm Limited 2020-12-17 Not applicable EU 
Azopt Suspension / drops 10 mg/1mL Ophthalmic Novartis Pharmaceuticals Corporation 1998-04-30 Not applicable US 
Azopt Suspension 1 % w/v Ophthalmic Novartis 1998-11-11 Not applicable Canada 
Azopt Suspension / drops 10 mg/ml Ophthalmic Novartis Europharm Limited 2020-12-17 Not applicable EU Azopt Suspension / drops 10 mg/1mL Ophthalmic ALCON LABORATORIES, INC. 1998-04-30 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Brinzolamide Suspension / drops 10 mg/1mL Ophthalmic Oceanside Pharmaceuticals. 2021-08-25 Not applicable US Brinzolamide Suspension / drops 10 mg/1mL Ophthalmic Sandoz Inc 2021-03-08 Not applicable US Brinzolamide Suspension / drops 10 mg/1mL Ophthalmic bryant ranch prepack 2021-03-08 Not applicable US Brinzolamide Suspension / drops 10 mg/1mL Ophthalmic Actavis Pharma, Inc. 2021-03-08 Not applicable US Sandoz Brinzolamide Suspension 1 % Ophthalmic Sandoz Canada Incorporated Not applicable Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Azarga Brinzolamide (10 mg/ml) + Timolol maleate (5 mg/ml) Suspension / drops Ophthalmic Novartis Europharm Limited 2016-09-20 Not applicable EU Azarga Brinzolamide (10 mg/ml) + Timolol maleate (5 mg/ml) Suspension / drops Ophthalmic Novartis Europharm Limited 2016-09-20 Not applicable EU Azarga Brinzolamide (1 % w/v) + Timolol maleate (0.5 % w/v) Suspension Ophthalmic Novartis 2009-08-25 Not applicable Canada AZARGA (EYE DROPS, SUSPENSION) Brinzolamide (10 MG/1ML) + Timolol (5 MG/1ML) Suspension / drops Ophthalmic บริษัท โนวาร์ตีส (ประเทศไทย) จำกัด 2017-09-07 Not applicable Thailand 
AZARGA 10 MG/ML+5 MG/ML STERİL SÜSPANSİYON GÖZ DAMLASI, 5 ML Brinzolamide (10 mg/ml) + Timolol (5 mg/ml) Suspension Ophthalmic NOVARTİS SAĞLIK GIDA VE TARIM ÜRÜNLERİ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey 
Azarga 10mg/mL + 5mg/mL eye drops, suspension Brinzolamide (10 mg/mL) + Timolol (5 mg/mL) Suspension Ophthalmic NOVARTIS (SINGAPORE) PTE LTD 2010-05-19 Not applicable Singapore BRİTİL-T 10 MG/ML + 5 MG/ML GÖZ DAMLASI, SÜSPANSİYON, 1 ADET Brinzolamide (10 mg/ml) + Timolol (5 mg/ml) Suspension / drops Ophthalmic World Medicine Ilac San. Ve Tic. a.s. 2020-08-14 Not applicable Turkey Simbrinza Brinzolamide (1 % w/v) + Brimonidine tartrate (0.2 % w/v) Suspension Ophthalmic Novartis 2015-02-17 Not applicable Canada Simbrinza Brinzolamide (10 mg/ml) + Brimonidine tartrate (2 mg/ml) Suspension / drops Ophthalmic Novartis Europharm Limited 2016-09-08 Not applicable EU Simbrinza Brinzolamide (10 mg/1mL) + Brimonidine tartrate (2 mg/1mL) Suspension / drops Ophthalmic Novartis Pharmaceuticals Corporation 2013-05-01 Not applicable US
Categories
- ATC Codes
- S01EC54 — Brinzolamide, combinations
- S01EC — Carbonic anhydrase inhibitors
- S01E — ANTIGLAUCOMA PREPARATIONS AND MIOTICS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- S01EC — Carbonic anhydrase inhibitors
- S01E — ANTIGLAUCOMA PREPARATIONS AND MIOTICS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- Drug Categories
- Amides
- Antiglaucoma Preparations and Miotics
- Carbonic Anhydrase Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Diuretics
- Enzyme Inhibitors
- Genito Urinary System and Sex Hormones
- Gynecological Antiinfectives and Antiseptics
- Ophthalmics
- Ophthalmologicals
- Sensory Organs
- Sulfonamides
- Sulfones
- Sulfur Compounds
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as thienothiazines. These are heterocyclic compounds containing a thiophene ring fused to a thiazine. Thiophene is 5-membered ring consisting of four carbon atoms and one sulfur atom. Thiazine is a 6-membered ring consisting of four carbon, one nitrogen and one sulfur atoms.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Thienothiazines
- Sub Class
- Not Available
- Direct Parent
- Thienothiazines
- Alternative Parents
- 2,3,5-trisubstituted thiophenes / Aralkylamines / Organosulfonamides / 1,2-thiazines / Heteroaromatic compounds / Aminosulfonyl compounds / Dialkylamines / Dialkyl ethers / Azacyclic compounds / Organopnictogen compounds show 2 more
- Substituents
- 2,3,5-trisubstituted thiophene / Amine / Aminosulfonyl compound / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Dialkyl ether / Ether / Heteroaromatic compound / Hydrocarbon derivative show 16 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- sulfonamide, thienothiazine (CHEBI:41212)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 9451Z89515
- CAS number
- 138890-62-7
- InChI Key
- HCRKCZRJWPKOAR-JTQLQIEISA-N
- InChI
- InChI=1S/C12H21N3O5S3/c1-3-14-10-8-15(5-4-6-20-2)23(18,19)12-9(10)7-11(21-12)22(13,16)17/h7,10,14H,3-6,8H2,1-2H3,(H2,13,16,17)/t10-/m0/s1
- IUPAC Name
- (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ⁶-thieno[3,2-e][1,2]thiazine-6-sulfonamide
- SMILES
- CCN[C@H]1CN(CCCOC)S(=O)(=O)C2=C1C=C(S2)S(N)(=O)=O
References
- Synthesis Reference
Alessandro Falchi, Ottorino De Lucchi, Andrea Castellin, "PROCESS FOR THE PREPARATION OF BRINZOLAMIDE." U.S. Patent US20110118461, issued May 19, 2011.
US20110118461- General References
- Ermis SS, Ozturk F, Inan UU: Comparing the effects of travoprost and brinzolamide on intraocular pressure after phacoemulsification. Eye (Lond). 2005 Mar;19(3):303-7. [Article]
- Iester M, Altieri M, Michelson G, Vittone P, Traverso CE, Calabria G: Retinal peripapillary blood flow before and after topical brinzolamide. Ophthalmologica. 2004 Nov-Dec;218(6):390-6. [Article]
- Kaup M, Plange N, Niegel M, Remky A, Arend O: Effects of brinzolamide on ocular haemodynamics in healthy volunteers. Br J Ophthalmol. 2004 Feb;88(2):257-62. [Article]
- Iester M: Brinzolamide ophthalmic suspension: a review of its pharmacology and use in the treatment of open angle glaucoma and ocular hypertension. Clin Ophthalmol. 2008 Sep;2(3):517-23. [Article]
- DeSantis L: Preclinical overview of brinzolamide. Surv Ophthalmol. 2000 Jan;44 Suppl 2:S119-29. [Article]
- FDA Approved Drug Products: AZOPT (brinzolamide) suspension [Link]
- FDA Approved Drug Products: SIMBRINZA (brinzolamide and brimonidine tartrate) suspension [Link]
- EMA Product Information: AZARGA (brinzolamide and timolol maleate) suspension [Link]
- External Links
- Human Metabolome Database
- HMDB0015325
- KEGG Drug
- D00652
- KEGG Compound
- C07760
- PubChem Compound
- 68844
- PubChem Substance
- 46507071
- ChemSpider
- 62077
- BindingDB
- 10885
- 194881
- ChEBI
- 3176
- ChEMBL
- CHEMBL220491
- ZINC
- ZINC000003953037
- Therapeutic Targets Database
- DAP000602
- PharmGKB
- PA164744929
- PDBe Ligand
- BZ1
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Brinzolamide
- PDB Entries
- 3znc / 4m2r / 4m2v / 6bbs
- FDA label
- Download (580 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Not Available Ocular Hypertension / Open Angle Glaucoma (OAG) 1 4 Completed Prevention Ocular Hypertension / Posterior Capsule Opacification 1 4 Completed Treatment Glaucoma 11 4 Completed Treatment Glaucoma / Ocular Hypertension 6 4 Completed Treatment Glaucoma / Ocular Hypertension / Open Angle Glaucoma (OAG) 1 4 Completed Treatment Infantile Nystagmus Syndrome 1 4 Completed Treatment Ocular Hypertension / Ocular Hypertension, Primary Open-angle Glaucoma (POAG) 2 4 Completed Treatment Ocular Hypertension / Ocular Hypertension, Primary Open-angle Glaucoma (POAG) / Pigment Dispersion Glaucoma 1 4 Completed Treatment Ocular Hypertension / Open Angle Glaucoma (OAG) 5 4 Completed Treatment Open Angle Glaucoma (OAG) 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Alcon Laboratories
- Dosage Forms
Form Route Strength Solution / drops Ophthalmic Solution / drops; suspension / drops Ophthalmic Suspension Ophthalmic Suspension Ophthalmic 10 mg/mL Solution / drops Ophthalmic Suspension Ophthalmic 1 % w/v Suspension / drops Ophthalmic 10 mg/1mL Solution / drops; suspension / drops Ophthalmic 10 MG/ML Suspension Ophthalmic Suspension Ophthalmic 10 MG/ML Solution Ophthalmic 10 mg/ml Suspension Conjunctival; Ophthalmic 10 mg Solution / drops Ophthalmic 10 MG/ML Suspension / drops Ophthalmic 10 mg/ml Suspension Ophthalmic 1 % Suspension / drops Ophthalmic Suspension Ophthalmic 2 mg/ml - Prices
Unit description Cost Unit Azopt 1% Suspension 15ml Bottle 163.11USD bottle Azopt 1% Suspension 10ml Bottle 108.83USD bottle Azopt 1% eye drops 8.05USD ml Azopt 1 % Suspension 3.63USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5461081 No 1995-10-24 2013-04-24 US US5240923 No 1993-08-31 2010-08-31 US CA2080223 No 2000-11-07 2011-04-03 Canada US6316441 No 2001-11-13 2019-12-07 US US9044484 No 2015-06-02 2030-10-30 US US9421265 No 2016-08-23 2030-06-17 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 131 °C Not Available logP -1.8 Not Available - Predicted Properties
Property Value Source Water Solubility 0.713 mg/mL ALOGPS logP -0.65 ALOGPS logP -0.67 ChemAxon logS -2.7 ALOGPS pKa (Strongest Acidic) 8.19 ChemAxon pKa (Strongest Basic) 6.78 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 6 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 118.8 Å2 ChemAxon Rotatable Bond Count 7 ChemAxon Refractivity 87.2 m3·mol-1 ChemAxon Polarizability 37.93 Å3 ChemAxon Number of Rings 2 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9765 Blood Brain Barrier + 0.8754 Caco-2 permeable - 0.7123 P-glycoprotein substrate Substrate 0.8185 P-glycoprotein inhibitor I Non-inhibitor 0.6795 P-glycoprotein inhibitor II Non-inhibitor 0.9245 Renal organic cation transporter Non-inhibitor 0.8276 CYP450 2C9 substrate Non-substrate 0.7897 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.6431 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8588 Ames test Non AMES toxic 0.5982 Carcinogenicity Non-carcinogens 0.7712 Biodegradation Not ready biodegradable 0.9834 Rat acute toxicity 2.4930 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7097 hERG inhibition (predictor II) Non-inhibitor 0.5167
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-000i-3940000000-29878662225bb11586ed
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Zinc ion binding
- Specific Function
- Essential for bone resorption and osteoclast differentiation (By similarity). Reversible hydration of carbon dioxide. Can hydrate cyanamide to urea. Involved in the regulation of fluid secretion in...
- Gene Name
- CA2
- Uniprot ID
- P00918
- Uniprot Name
- Carbonic anhydrase 2
- Molecular Weight
- 29245.895 Da
References
- Stams T, Chen Y, Boriack-Sjodin PA, Hurt JD, Liao J, May JA, Dean T, Laipis P, Silverman DN, Christianson DW: Structures of murine carbonic anhydrase IV and human carbonic anhydrase II complexed with brinzolamide: molecular basis of isozyme-drug discrimination. Protein Sci. 1998 Mar;7(3):556-63. [Article]
- DeSantis L: Preclinical overview of brinzolamide. Surv Ophthalmol. 2000 Jan;44 Suppl 2:S119-29. [Article]
- Winum JY, Casini A, Mincione F, Starnotti M, Montero JL, Scozzafava A, Supuran CT: Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-alpha-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits. Bioorg Med Chem Lett. 2004 Jan 5;14(1):225-9. [Article]
- Boriack-Sjodin PA, Zeitlin S, Chen HH, Crenshaw L, Gross S, Dantanarayana A, Delgado P, May JA, Dean T, Christianson DW: Structural analysis of inhibitor binding to human carbonic anhydrase II. Protein Sci. 1998 Dec;7(12):2483-9. [Article]
- Ilies M, Supuran CT, Scozzafava A, Casini A, Mincione F, Menabuoni L, Caproiu MT, Maganu M, Banciu MD: Carbonic anhydrase inhibitors: sulfonamides incorporating furan-, thiophene- and pyrrole-carboxamido groups possess strong topical intraocular pressure lowering properties as aqueous suspensions. Bioorg Med Chem. 2000 Aug;8(8):2145-55. [Article]
- Iester M: Brinzolamide ophthalmic suspension: a review of its pharmacology and use in the treatment of open angle glaucoma and ocular hypertension. Clin Ophthalmol. 2008 Sep;2(3):517-23. [Article]
- Vullo D, Franchi M, Gallori E, Antel J, Scozzafava A, Supuran CT: Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides. J Med Chem. 2004 Feb 26;47(5):1272-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Zinc ion binding
- Specific Function
- Reversible hydration of carbon dioxide. Can hydrates cyanamide to urea.
- Gene Name
- CA1
- Uniprot ID
- P00915
- Uniprot Name
- Carbonic anhydrase 1
- Molecular Weight
- 28870.0 Da
References
- Winum JY, Casini A, Mincione F, Starnotti M, Montero JL, Scozzafava A, Supuran CT: Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-alpha-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits. Bioorg Med Chem Lett. 2004 Jan 5;14(1):225-9. [Article]
- Herkel U, Pfeiffer N: Update on topical carbonic anhydrase inhibitors. Curr Opin Ophthalmol. 2001 Apr;12(2):88-93. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Zinc ion binding
- Specific Function
- Reversible hydration of carbon dioxide. May stimulate the sodium/bicarbonate transporter activity of SLC4A4 that acts in pH homeostasis. It is essential for acid overload removal from the retina an...
- Gene Name
- CA4
- Uniprot ID
- P22748
- Uniprot Name
- Carbonic anhydrase 4
- Molecular Weight
- 35032.075 Da
References
- Vullo D, Franchi M, Gallori E, Antel J, Scozzafava A, Supuran CT: Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides. J Med Chem. 2004 Feb 26;47(5):1272-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Zinc ion binding
- Specific Function
- Reversible hydration of carbon dioxide. Low activity.
- Gene Name
- CA5A
- Uniprot ID
- P35218
- Uniprot Name
- Carbonic anhydrase 5A, mitochondrial
- Molecular Weight
- 34750.21 Da
References
- Vullo D, Franchi M, Gallori E, Antel J, Scozzafava A, Supuran CT: Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides. J Med Chem. 2004 Feb 26;47(5):1272-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Zinc ion binding
- Specific Function
- Reversible hydration of carbon dioxide.
- Gene Name
- CA3
- Uniprot ID
- P07451
- Uniprot Name
- Carbonic anhydrase 3
- Molecular Weight
- 29557.215 Da
References
- Nishimori I, Minakuchi T, Onishi S, Vullo D, Cecchi A, Scozzafava A, Supuran CT: Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. Bioorg Med Chem. 2007 Dec 1;15(23):7229-36. Epub 2007 Aug 25. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
Drug created at June 13, 2005 13:24 / Updated at January 27, 2022 17:28