Banner
targets (31) enzymes (3)
for drugs
Identification
Name Zonisamide
Accession Number DB00909 (APRD00004)
Type small molecule
Groups approved
Description

Zonisamide is a sulfonamide anticonvulsant approved for use as an adjunctive therapy in adults with partial-onset seizures. Zonisamide may be a carbonic anhydrase inhibitor although this is not one of the primary mechanisms of action. 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.
Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms
Zonisamida [Spanish]
Zonisamidum [Latin]
Salts Not Available
Brand names
Name Company
Exceglan
Excegram
Excegran
Zonegran
Brand mixtures Not Available
Categories
  • Antioxidants
  • Anticonvulsants
CAS number 68291-97-4
Weight Average: 212.226
Monoisotopic: 212.025562822
Chemical Formula C8H8N2O3S
InChI Key InChIKey=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)
Plain Text
IUPAC Name
1,2-benzoxazol-3-ylmethanesulfonamide
SMILES
NS(=O)(=O)CC1=NOC2=CC=CC=C12
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Organic
Classes
  • Benzoxazoles
Substructures
  • Sulfonyls
  • Benzene and Derivatives
  • Isoxazoles
  • Heterocyclic compounds
  • Aromatic compounds
  • Oxazoles
  • Sulfonamides
  • Imines
  • Benzoxazoles
Pharmacology
Indication For use as adjunctive treatment of partial seizures in adults with epilepsy.
Pharmacodynamics Zonisamide is an antiseizure drug chemically classified as a sulfonamide and unrelated to other antiseizure agents. The precise mechanism by which zonisamide exerts its antiseizure effect is unknown, although it is believed that the drug blocks sodium and calcium channels, which leads to the suppression of neuronal hypersynchronization (i.e. convulsions). Sonisamide has also been found to potentiate dopaminergic and serotonergic neurotransmission but does not appear to potentiate syanptic activity by GABA (gamma amino butyric acid).
Mechanism of action Zonisamide binds to sodium channels and voltage sensitive calcium channels, which suppresses neuronal depolarization and hypersynchronization. Zonisamide also inhibits carbonic anhydrase to a weaker extent, but such an effect is not thought to contribute substantially to the drug's anticonvulsant activity.
Absorption Variable, yet relatively rapid rate of absorption with a time to peak concentration of 2.8-3.9 hours. Food has no effect on the bioavailability of zonisamide.
Volume of distribution
  • 1.45 L/kg
Protein binding 40% (at concentrations of 1.0-7.0 µg/mL)
Metabolism Primarily hepatic through cytochrome P450 isoenzyme 3A4 (CYP3A4). Undergoes acetylation and reduction, forming N-acetyl zonisamide, and the open-ring metabolite 2–sulfamoylacetyl phenol, respectively.
Route of elimination Zonisamide is excreted primarily in urine as parent drug and as the glucuronide of a metabolite.
Half life 63 hours
Clearance
  • 0.30 – 0.35 mL/min/kg [patients not receiving enzyme-inducing antiepilepsy drugs (AEDs)]
  • 0.35 – 0.5 mL/min/kg [Concomitant administration of phenytoin and carbamazepine]
Toxicity Symptoms of overdose include diminished breathing, loss of consciousness, low blood pressure, and slow heartbeat.
Affected organisms
  • Humans and other mammals
Pathways Not Available
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
Dosage forms
Form Route Strength
Capsule Oral
Prices
Unit description Cost Unit
Zonegran 100 mg capsule 3.33 USD capsule
Zonisamide 100 mg capsule 2.24 USD capsule
Zonegran 50 mg capsule 1.22 USD capsule
Zonisamide 50 mg capsule 1.12 USD capsule
Zonegran 25 mg capsule 0.94 USD capsule
Zonisamide 25 mg capsule 0.56 USD capsule
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 161-163 °C Not Available
water solubility 0.8 mg/mL Not Available
logP 0.5 Not Available
pKa 10.2 Not Available
Predicted Properties
Property Value Source
water solubility 2.09e+00 g/l ALOGPS
logP 0.67 ALOGPS
logP 0.11 ChemAxon
logS -2 ALOGPS
pKa (strongest acidic) 9.84 ChemAxon
pKa (strongest basic) -1.8 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 86.19 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 50.3 ChemAxon
polarizability 19.48 ChemAxon
References
Synthesis Reference Not Available
General Reference
  1. Murata M, Horiuchi E, Kanazawa I: Zonisamide has beneficial effects on Parkinson’s disease patients. Neurosci Res. 2001 Dec;41(4):397-9. Pubmed
  2. Gadde KM, Franciscy DM, Wagner HR 2nd, Krishnan KR: Zonisamide for weight loss in obese adults: a randomized controlled trial. JAMA. 2003 Apr 9;289(14):1820-5. Pubmed
  3. Hasegawa H: Utilization of zonisamide in patients with chronic pain or epilepsy refractory to other treatments: a retrospective, open label, uncontrolled study in a VA hospital. Curr Med Res Opin. 2004 May;20(5):577-80. Pubmed
  4. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  5. 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. Pubmed
  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. Pubmed
  7. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  8. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. Pubmed
  9. 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. Pubmed
  10. 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. Pubmed
External Links
Resource Link
KEGG Drug D00538 Link_out
KEGG Compound C07504 Link_out
PubChem Compound 5734 Link_out
PubChem Substance 46505278 Link_out
ChemSpider 5532 Link_out
BindingDB 10888 Link_out
ChEBI 10127 Link_out
ChEMBL 10127 Link_out
Therapeutic Targets Database DAP000500 Link_out
PharmGKB PA451978 Link_out
RxList http://www.rxlist.com/cgi/generic3/zonisamide.htm Link_out
Drugs.com http://www.drugs.com/cdi/zonisamide.html Link_out
PDRhealth http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/zon1564.shtml Link_out
Wikipedia http://en.wikipedia.org/wiki/Zonisamide Link_out
ATC Codes
  • N03AX15
AHFS Codes Not Available
PDB Entries Not Available
FDA label show (124 KB)
MSDS show (58.3 KB)
Interactions
Drug Interactions
Drug Interaction
Amprenavir Amprenavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if amprenavir is initiated, discontinued or dose changed.
Atazanavir Atazanavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if atazanavir is initiated, discontinued or dose changed.
Brinzolamide As both brinzolamide and zonisamide are carbonic anhydrase inhibitors, there is an increased risk of adverse effects.The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Avoid concurrent use of different carbonic anhydrase inhibitors when possible.
Clarithromycin Clarithromcyin, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if clarithromycin is initiated, discontinued or dose changed.
Conivaptan Conivaptan, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if conivaptan is initiated, discontinued or dose changed.
Darunavir Darunavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if darunavir is initiated, discontinued or dose changed.
Delavirdine Delavirdine, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if delavirdine is initiated, discontinued or dose changed.
Fosamprenavir Fosamprenavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if fosamprenavir is initiated, discontinued or dose changed.
Imatinib Imatinib, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if imatinib is initiated, discontinued or dose changed.
Indinavir Indinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if indinavir is initiated, discontinued or dose changed.
Isoniazid Isoniazid, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if isoniazid is initiated, discontinued or dose changed.
Itraconazole Itraconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if itraconazole is initiated, discontinued or dose changed.
Ketoconazole Ketonconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if ketoconazole is initiated, discontinued or dose changed.
Lopinavir Lopinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if lopinavir is initiated, discontinued or dose changed.
Mefloquine Mefloquine may decrease the serum concentration and therapeutic effect of zonisamide. Concomitant therapy is contraindicated in patients with history of convulsions.
Methotrimeprazine Additive CNS depressant effects. Reduce zonisamide dose by half upon initiation of methotrimeprazine. Zonisamide dose may be adjusted once methotrimeprazine dose has been established. Monitor for increased CNS depression.
Nefazodone Nefazodone, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if nefazodone is initiated, discontinued or dose changed.
Nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if nelfinavir is initiated, discontinued or dose changed.
Nicardipine Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if nicardipine is initiated, discontinued or dose changed.
Posaconazole Posaconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if posaconazole is initiated, discontinued or dose changed.
Quinidine Quinidine, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if quinidine is initiated, discontinued or dose changed.
Ritonavir Ritonavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if ritonavir is initiated, discontinued or dose changed.
Saquinavir Saquinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if saquinavir is initiated, discontinued or dose changed.
Telithromycin Telithromycin, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if telithromycin is initiated, discontinued or dose changed.
Triprolidine The CNS depressants, Triprolidine and Zonisamide, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if voriconazole is initiated, discontinued or dose changed.
Food Interactions Not Available
Targets

1. Sodium channel protein type 1 subunit alpha

Pharmacological action: yes
Actions: inhibitor

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

Organism class: human
UniProt ID: P35498 Link_out
Gene: SCN1A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  2. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  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. Pubmed
  8. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Sodium channel protein type 2 subunit alpha

Pharmacological action: yes
Actions: inhibitor

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

Organism class: human
UniProt ID: Q99250 Link_out
Gene: SCN2A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  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. Pubmed

3. Sodium channel protein type 3 subunit alpha

Pharmacological action: yes
Actions: inhibitor

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

Organism class: human
UniProt ID: Q9NY46 Link_out
Gene: SCN3A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  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. Pubmed

4. Sodium channel protein type 4 subunit alpha

Pharmacological action: yes
Actions: inhibitor

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. This sodium channel may be present in both denervated and innervated skeletal muscle

Organism class: human
UniProt ID: P35499 Link_out
Gene: SCN4A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  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. Pubmed

5. Sodium channel protein type 5 subunit alpha

Pharmacological action: yes
Actions: inhibitor

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. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is responsible for the initial upstroke of the action potential in the electrocardiogram

Organism class: human
UniProt ID: Q14524 Link_out
Gene: SCN5A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  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. Pubmed

6. Sodium channel protein type 9 subunit alpha

Pharmacological action: yes
Actions: inhibitor

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. It is a tetrodotoxin-sensitive Na(+) channel isoform. Plays a role in pain mechanisms, especially in the development of inflammatory pain

Organism class: human
UniProt ID: Q15858 Link_out
Gene: SCN9A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  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. Pubmed

7. Sodium channel protein type 11 subunit alpha

Pharmacological action: yes
Actions: inhibitor

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 sodium ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant sodium channel isoform. Also involved, with the contribution of the receptor tyrosine kinase NTRK2, in rapid BDNF-evoked neuronal depolarization

Organism class: human
UniProt ID: Q9UI33 Link_out
Gene: SCN11A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  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. Pubmed

8. Sodium channel subunit beta-1

Pharmacological action: yes
Actions: inhibitor

Crucial in the assembly, expression, and functional modulation of the heterotrimeric complex of the sodium channel. The subunit beta-1 can modulate multiple alpha subunit isoforms from brain, skeletal muscle, and heart. Its association with neurofascin may target the sodium channels to the nodes of Ranvier of developing axons and retain these channels at the nodes in mature myelinated axons

Organism class: human
UniProt ID: Q07699 Link_out
Gene: SCN1B Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  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. Pubmed

9. Sodium channel subunit beta-2

Pharmacological action: yes
Actions: inhibitor

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)

Organism class: human
UniProt ID: O60939 Link_out
Gene: SCN2B Link_out
Protein Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  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. Pubmed

10. Sodium channel subunit beta-3

Pharmacological action: yes
Actions: inhibitor

Modulates channel gating kinetics. Causes unique persistent sodium currents. Inactivates the sodium channel opening more slowly than the subunit beta-1. Its association with neurofascin 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)

Organism class: human
UniProt ID: Q9NY72 Link_out
Gene: SCN3B Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  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. Pubmed

11. Sodium channel subunit beta-4

Pharmacological action: yes
Actions: inhibitor

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 (By similarity)

Organism class: human
UniProt ID: Q8IWT1 Link_out
Gene: SCN4B Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  3. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  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. Pubmed

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

Pharmacological action: yes
Actions: inhibitor

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 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

Organism class: human
UniProt ID: O43497 Link_out
Gene: CACNA1G Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. 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. Pubmed
  3. Kothare SV, Kaleyias J: Zonisamide: review of pharmacology, clinical efficacy, tolerability, and safety. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):493-506. Pubmed
  4. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  5. 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. Pubmed
  6. Janszky J: [Role of zonisamid in treating epilepsy, Parkinson disorders and other neurological diseases] Ideggyogy Sz. 2009 Nov 30;62(11-12):383-9. Pubmed
  7. 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. Epub 2009 Dec 4. Pubmed
  8. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  9. Murata M: Novel therapeutic effects of the anti-convulsant, zonisamide, on Parkinson’s disease. Curr Pharm Des. 2004;10(6):687-93. Pubmed
  10. Murata M: Zonisamide: a new drug for Parkinson’s disease. Drugs Today (Barc). 2010 Apr;46(4):251-8. Pubmed
  11. 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. Pubmed
  12. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed

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

Pharmacological action: yes
Actions: inhibitor

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-1H 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

Organism class: human
UniProt ID: O95180 Link_out
Gene: CACNA1H Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  7. Murata M: Novel therapeutic effects of the anti-convulsant, zonisamide, on Parkinson’s disease. Curr Pharm Des. 2004;10(6):687-93. Pubmed
  8. Murata M: Zonisamide: a new drug for Parkinson’s disease. Drugs Today (Barc). 2010 Apr;46(4):251-8. Pubmed
  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. Pubmed
  10. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed

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

Pharmacological action: yes
Actions: inhibitor

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. Isoform alpha-1I 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

Organism class: human
UniProt ID: Q9P0X4 Link_out
Gene: CACNA1I Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Epub 2009 Dec 4. Pubmed
  6. Leppik IE: Zonisamide: chemistry, mechanism of action, and pharmacokinetics. Seizure. 2004 Dec;13 Suppl 1:S5-9; discussion S10. Pubmed
  7. Murata M: Novel therapeutic effects of the anti-convulsant, zonisamide, on Parkinson’s disease. Curr Pharm Des. 2004;10(6):687-93. Pubmed
  8. Murata M: Zonisamide: a new drug for Parkinson’s disease. Drugs Today (Barc). 2010 Apr;46(4):251-8. Pubmed
  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. Pubmed
  10. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed

15. Carbonic anhydrase 1

Pharmacological action: unknown
Actions: inhibitor

Reversible hydration of carbon dioxide

Organism class: human
UniProt ID: P00915 Link_out
Gene: CA1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Masuda Y, Karasawa T: Inhibitory effect of zonisamide on human carbonic anhydrase in vitro. Arzneimittelforschung. 1993 Apr;43(4):416-8. Pubmed
  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. Pubmed
  6. Temperini C, Cecchi A, Boyle NA, Scozzafava A, Cabeza JE, Wentworth P Jr, Blackburn GM, Supuran CT: Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. Bioorg Med Chem Lett. 2008 Feb 1;18(3):999-1005. Epub 2007 Dec 15. Pubmed
  7. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  8. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

16. Carbonic anhydrase 2

Pharmacological action: unknown
Actions: inhibitor

Reversible hydration of carbon dioxide

Organism class: human
UniProt ID: P00918 Link_out
Gene: CA2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  5. Masuda Y, Karasawa T: Inhibitory effect of zonisamide on human carbonic anhydrase in vitro. Arzneimittelforschung. 1993 Apr;43(4):416-8. Pubmed
  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. Pubmed
  7. Temperini C, Cecchi A, Boyle NA, Scozzafava A, Cabeza JE, Wentworth P Jr, Blackburn GM, Supuran CT: Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. Bioorg Med Chem Lett. 2008 Feb 1;18(3):999-1005. Epub 2007 Dec 15. Pubmed
  8. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  9. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

17. Carbonic anhydrase 3

Pharmacological action: unknown
Actions: inhibitor

Reversible hydration of carbon dioxide

Organism class: human
UniProt ID: P07451 Link_out
Gene: CA3 Link_out
Protein Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Temperini C, Cecchi A, Boyle NA, Scozzafava A, Cabeza JE, Wentworth P Jr, Blackburn GM, Supuran CT: Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. Bioorg Med Chem Lett. 2008 Feb 1;18(3):999-1005. Epub 2007 Dec 15. Pubmed
  5. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  6. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

18. Carbonic anhydrase 4

Pharmacological action: unknown
Actions: inhibitor

Reversible hydration of carbon dioxide. May stimulate the sodium/bicarbonate transporter activity of SLC4A4

Organism class: human
UniProt ID: P22748 Link_out
Gene: CA4 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  5. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

19. Carbonic anhydrase 5A, mitochondrial

Pharmacological action: unknown
Actions: inhibitor

Reversible hydration of carbon dioxide

Organism class: human
UniProt ID: P35218 Link_out
Gene: CA5A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  5. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  6. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

20. Carbonic anhydrase 5B, mitochondrial

Pharmacological action: unknown
Actions: inhibitor

Reversible hydration of carbon dioxide

Organism class: human
UniProt ID: Q9Y2D0 Link_out
Gene: CA5B Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  5. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  6. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

21. Carbonic anhydrase 6

Pharmacological action: unknown
Actions: inhibitor
Organism class: human
UniProt ID: P23280 Link_out
Gene: CA6
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  5. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

22. Carbonic anhydrase 7

Pharmacological action: unknown
Actions: inhibitor

Reversible hydration of carbon dioxide

Organism class: human
UniProt ID: P43166 Link_out
Gene: CA7 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  5. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

23. Carbonic anhydrase-related protein

Pharmacological action: unknown
Actions: inhibitor

Does not have a carbonic anhydrase catalytic activity

Organism class: human
UniProt ID: P35219 Link_out
Gene: CA8 Link_out
Protein Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  5. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

24. Carbonic anhydrase 9

Pharmacological action: unknown
Actions: inhibitor

Reversible hydration of carbon dioxide. May be involved in the control of cell proliferation and transformation. Appears to be a novel specific biomarker for a cervical neoplasia

Organism class: human
UniProt ID: Q16790 Link_out
Gene: CA9
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  5. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

25. Carbonic anhydrase-related protein 10

Pharmacological action: unknown
Actions: inhibitor

Does not have a catalytic activity

Organism class: human
UniProt ID: Q9NS85 Link_out
Gene: CA10 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  5. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

26. Carbonic anhydrase-related protein 11

Pharmacological action: unknown
Actions: inhibitor

Does not have a catalytic activity

Organism class: human
UniProt ID: O75493 Link_out
Gene: CA11 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  5. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

27. Carbonic anhydrase 12

Pharmacological action: unknown
Actions: inhibitor

Reversible hydration of carbon dioxide

Organism class: human
UniProt ID: O43570 Link_out
Gene: CA12 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  5. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

28. Carbonic anhydrase 13

Pharmacological action: unknown
Actions: inhibitor

Reversible hydration of carbon dioxide

Organism class: human
UniProt ID: Q8N1Q1 Link_out
Gene: CA13 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  5. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

29. Carbonic anhydrase 14

Pharmacological action: unknown
Actions: inhibitor

Reversible hydration of carbon dioxide

Organism class: human
UniProt ID: Q9ULX7 Link_out
Gene: CA14 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Biton V: Clinical pharmacology and mechanism of action of zonisamide. Clin Neuropharmacol. 2007 Jul-Aug;30(4):230-40. Pubmed
  5. Zonisamide: new drug. No advantage in refractory partial epilepsy. Prescrire Int. 2007 Jun;16(89):95-7. Pubmed

30. Amine oxidase [flavin-containing] B

Pharmacological action: unknown
Actions: inhibitor

Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOB preferentially degrades benzylamine and phenylethylamine

Organism class: human
UniProt ID: P27338 Link_out
Gene: MAOB Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Epub 2009 Dec 4. Pubmed
  2. Murata M: Novel therapeutic effects of the anti-convulsant, zonisamide, on Parkinson’s disease. Curr Pharm Des. 2004;10(6):687-93. Pubmed
  3. Murata M, Horiuchi E, Kanazawa I: Zonisamide has beneficial effects on Parkinson’s disease patients. Neurosci Res. 2001 Dec;41(4):397-9. Pubmed
  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. Pubmed
  5. Murata M: Zonisamide: a new drug for Parkinson’s disease. Drugs Today (Barc). 2010 Apr;46(4):251-8. Pubmed
  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. Pubmed
  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. Pubmed

31. Amine oxidase [flavin-containing] A

Pharmacological action: unknown
Actions: inhibitor

Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOA preferentially oxidizes biogenic amines such as 5-hydroxytryptamine (5-HT), norepinephrine and epinephrine

Organism class: human
UniProt ID: P21397 Link_out
Gene: MAOA Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Pubmed
  2. Murata M: Zonisamide: a new drug for Parkinson’s disease. Drugs Today (Barc). 2010 Apr;46(4):251-8. Pubmed
Enzymes

1. Cytochrome P450 3A4

Actions: substrate

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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4- hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. The enzyme also hydroxylates etoposide

UniProt ID: P08684 Link_out
Gene: CYP3A4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Nakasa H, Komiya M, Ohmori S, Rikihisa T, Kiuchi M, Kitada M: Characterization of human liver microsomal cytochrome P450 involved in the reductive metabolism of zonisamide. Mol Pharmacol. 1993 Jul;44(1):216-21. Pubmed
  2. Schulze-Bonhage A: Zonisamide in the treatment of epilepsy. Expert Opin Pharmacother. 2010 Jan;11(1):115-26. Pubmed
  3. 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. Pubmed
  4. Nakasa H, Nakamura H, Ono S, Tsutsui M, Kiuchi M, Ohmori S, Kitada M: Prediction of drug-drug interactions of zonisamide metabolism in humans from in vitro data. Eur J Clin Pharmacol. 1998 Apr;54(2):177-83. Pubmed
  5. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

2. Aldehyde oxidase

Actions: substrate

An aldehyde + H(2)O + O(2) = a carboxylic acid + H(2)O(2)

UniProt ID: Q06278 Link_out
Gene: AOX1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Sugihara K, Kitamura S, Tatsumi K: Involvement of mammalian liver cytosols and aldehyde oxidase in reductive metabolism of zonisamide. Drug Metab Dispos. 1996 Feb;24(2):199-202. Pubmed
  2. Kitamura S, Ohashi KNK, Sugihara K, Hosokawa R, Akagawa Y, Ohta S: Extremely high drug-reductase activity based on aldehyde oxidase in monkey liver. Biol Pharm Bull. 2001 Jul;24(7):856-9. Pubmed

3. Cytochrome P450 2C19

Actions: inhibitor

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

UniProt ID: P33261 Link_out
Gene: CYP2C19 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
Comments
Drug created on June 13, 2005 07:24 / Updated on February 08, 2013 16:19