Identification

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Name
Zolmitriptan
Accession Number
DB00315  (APRD00376)
Type
Small Molecule
Groups
Approved, Investigational
Description

Zolmitriptan is a synthetic tryptamine derivative readily soluble in water.

Structure
Thumb
Synonyms
  • (S)-4-({3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}methyl)-1,3-oxazolidin-2-one
  • 4-[[3-(2-dimethylaminoethyl)-1H-indol-5-yl]methyl]oxazolidin-2-one
  • Zolmitriptan
  • Zolmitriptán
  • Zolmitriptanum
External IDs
311 C 90 / BW 311 C 90
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Nra-zolmitriptanTabletOralNora Pharma IncNot applicableNot applicableCanada
ZolmitriptanTablet2.5 mgOralPro Doc Limitee2012-03-29Not applicableCanada
ZolmitriptanTablet5 mg/1OralImpax Generics2013-05-142019-10-31Us
ZolmitriptanTablet2.5 mg/1OralImpax Generics2013-05-142019-03-31Us0115 067120180913 8702 1n44oqt
ZolmitriptanTablet2.5 mgOralSanis Health Inc2015-10-14Not applicableCanada
ZolmitriptanTablet2.5 mgOralJubilant Generics LimitedNot applicableNot applicableCanada
Zolmitriptan ODTTablet, orally disintegratingOralSanis Health Inc2015-10-14Not applicableCanada
Zolmitriptan ODTTablet, orally disintegratingOralPro Doc Limitee2012-03-29Not applicableCanada
Zolmitriptan Orally DisintegratingTablet, orally disintegrating5 mg/1OralImpax Generics2013-05-142019-08-31Us
Zolmitriptan Orally DisintegratingTablet, orally disintegrating2.5 mg/1OralImpax Generics2013-05-142020-08-31Us
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ag-zolmitriptan ODTTablet, orally disintegratingOralAngita Pharma Inc.2015-12-10Not applicableCanada
Apo-zolmitriptanTabletOralApotex Corporation2016-08-15Not applicableCanada
Apo-zolmitriptan RapidTablet, orally disintegratingOralApotex Corporation2016-07-22Not applicableCanada
Auro-zolmitriptanTabletOralAuro Pharma IncNot applicableNot applicableCanada
Ccp-zolmitriptanTabletOralCellchem Pharmaceuticals Inc.2019-01-04Not applicableCanada
Dom-zolmitriptanTabletOralDominion Pharmacal2013-03-12Not applicableCanada
Dom-zolmitriptan ODTTablet, orally disintegratingOralDominion PharmacalNot applicableNot applicableCanada
Ipg-zolmitriptanTabletOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Jamp ZolmitriptanTabletOralJamp Pharma CorporationNot applicableNot applicableCanada
Jamp-zolmitriptanTabletOralJamp Pharma Corporation2014-03-13Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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International/Other Brands
AscoTop (AstraZeneca) / Nomi (Square) / Zipton / Zolmiles (Actavis) / Zolmit (Beximco) / Zomigon (AstraZeneca) / Zomigoro (AstraZeneca) / Zomitan (Incepta)
Categories
UNII
2FS66TH3YW
CAS number
139264-17-8
Weight
Average: 287.3568
Monoisotopic: 287.163376931
Chemical Formula
C16H21N3O2
InChI Key
ULSDMUVEXKOYBU-ZDUSSCGKSA-N
InChI
InChI=1S/C16H21N3O2/c1-19(2)6-5-12-9-17-15-4-3-11(8-14(12)15)7-13-10-21-16(20)18-13/h3-4,8-9,13,17H,5-7,10H2,1-2H3,(H,18,20)/t13-/m0/s1
IUPAC Name
(4S)-4-({3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}methyl)-1,3-oxazolidin-2-one
SMILES
CN(C)CCC1=CNC2=CC=C(C[C@H]3COC(=O)N3)C=C12

Pharmacology

Indication

For the acute treatment of adult migraine with or without auras.

Associated Conditions
Pharmacodynamics

Zolmitriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonists, and has only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Zolmitriptan also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Zolmitriptan in humans.

Mechanism of action

Zolmitriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of zolmitriptan for the treatment of migraine headache can most likely be attributed to the agonist effects at the 5HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.

TargetActionsOrganism
A5-hydroxytryptamine receptor 1B
agonist
Humans
A5-hydroxytryptamine receptor 1D
agonist
Humans
A5-hydroxytryptamine receptor 1F
agonist
Humans
A5-hydroxytryptamine receptor 1A
agonist
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Mean absolute oral bioavailability is approximately 40%. Food has no affect on the rate and extent of absorption.

Volume of distribution
  • 8.4±3.3 L/kg
Protein binding

25%

Metabolism

Hepatic. There have been three metabolites identified: indole acetic acid, N -oxide, and N-desmethyl metabolites. However, the N-desmethyl is the only active metabolite.

Route of elimination
Not Available
Half life

The mean elimination half-life of zolmitriptan and of the active N-desmethyl metabolite is 3 hours.

Clearance
  • 25.9 mL/min/kg
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3---(C;T) / (T;T)T AlleleEffect Directly StudiedPatients with this genotype have an increased likelihood of responding to zolmitriptan when treating (condition: cluster headache).Details

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.
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Zolmitriptan.
(S)-WarfarinThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with (S)-Warfarin.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic AcidThe risk or severity of hypertension can be increased when Zolmitriptan is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
1-benzylimidazoleThe risk or severity of hypertension can be increased when Zolmitriptan is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Zolmitriptan is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarinThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with 4-hydroxycoumarin.
4-MethoxyamphetamineThe metabolism of Zolmitriptan can be decreased when combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with 5-methoxy-N,N-dimethyltryptamine.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

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  • Action
    Action

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Food Interactions
Not Available

References

Synthesis Reference

Islam Aminul, Bhar Chandan, Katam Sahadev, "Process for preparing optically pure zolmitriptan." U.S. Patent US20050245585, issued November 03, 2005.

US20050245585
General References
  1. Pascual J: [Mechanism of action of zolmitriptan]. Neurologia. 1998 Oct;13 Suppl 2:9-15. [PubMed:9859690]
  2. Martin GR: Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine. Cephalalgia. 1997 Oct;17 Suppl 18:4-14. [PubMed:9399012]
External Links
Human Metabolome Database
HMDB0014460
KEGG Drug
D00415
KEGG Compound
C07218
PubChem Compound
60857
PubChem Substance
46506452
ChemSpider
54844
BindingDB
50033383
ChEBI
10124
ChEMBL
CHEMBL1185
Therapeutic Targets Database
DAP000077
PharmGKB
PA451975
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Zolmitriptan
ATC Codes
N02CC03 — Zolmitriptan
AHFS Codes
  • 28:32.28 — Selective Serotonin Agonists
FDA label
Download (101 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceMigraine1
1CompletedTreatmentMigraine4
2, 3CompletedTreatmentAcute Migraine1
2, 3RecruitingTreatmentCluster Headache1
3CompletedTreatmentMigraine4
4CompletedOtherWorkplace Migraine Treatment1
4CompletedTreatmentAcute Migraine1
4CompletedTreatmentMigraine2
4Not Yet RecruitingTreatmentCluster Headache1
Not AvailableCompletedNot AvailableMigraine Disorders3
Not AvailableCompletedTreatmentAcute Migraine / Headache Disorders / Migraine1

Pharmacoeconomics

Manufacturers
  • Astrazeneca pharmaceuticals lp
  • Ipr pharmaceuticals inc
Packagers
  • AstraZeneca Inc.
  • Cima Laboratories Inc.
  • IPR Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Promex Medical Inc.
  • Stat Rx Usa
Dosage forms
FormRouteStrength
Tablet, orally disintegratingOral
Tablet, multilayer, extended releaseOral
TabletOral
TabletOral2.5 mg
Tablet, film coatedOral2.5 mg/1
Tablet, film coatedOral5 mg/1
Spray, meteredNasal2.5 mg/1
Spray, meteredNasal5 mg/1
TabletOral2.5 mg/1
TabletOral5 mg/1
SprayNasal; Oral
Tablet, orally disintegratingOral2.5 mg/1
Tablet, orally disintegratingOral5 mg/1
Prices
Unit descriptionCostUnit
Zomig 6 5 mg Solution 1 Box = 6 Single Use Bottles235.62USD bottle
Zomig ZMT 6 2.5 mg Dispersible Tablet Box159.66USD box
Zomig 6 2.5 mg tablet 1 Box = 6 tablet147.23USD box
Zomig 3 5 mg tablet Box93.49USD box
Zomig ZMT 3 5 mg Dispersible Tablet Box88.21USD box
Zomig 5 mg nasal spray37.76USD each
Zomig 5 mg tablet28.82USD tablet
Zomig zmt 5 mg tablet28.27USD tablet
Zomig 2.5 mg tablet26.08USD tablet
Zomig zmt 2.5 mg tablet25.59USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5466699No1995-11-142012-11-14Us
CA2572508No2010-03-302016-08-02Canada
CA2064815No1999-11-162011-06-06Canada
US7220767Yes2007-05-222021-05-28Us
US6750237Yes2004-06-152021-05-28Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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Properties

State
Solid
Experimental Properties
PropertyValueSource
logP1.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.19 mg/mLALOGPS
logP2.25ALOGPS
logP2.04ChemAxon
logS-3.2ALOGPS
pKa (Strongest Acidic)13ChemAxon
pKa (Strongest Basic)9.55ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area57.36 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity82.44 m3·mol-1ChemAxon
Polarizability31.65 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.8956
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.6888
P-glycoprotein inhibitor INon-inhibitor0.8782
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterNon-inhibitor0.7674
CYP450 2C9 substrateNon-substrate0.8051
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.5822
CYP450 1A2 substrateNon-inhibitor0.6189
CYP450 2C9 inhibitorNon-inhibitor0.8989
CYP450 2D6 inhibitorNon-inhibitor0.8281
CYP450 2C19 inhibitorNon-inhibitor0.831
CYP450 3A4 inhibitorNon-inhibitor0.8481
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9263
Ames testNon AMES toxic0.7651
CarcinogenicityNon-carcinogens0.9641
BiodegradationNot ready biodegradable0.9961
Rat acute toxicity2.5965 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9301
hERG inhibition (predictor II)Non-inhibitor0.8949
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-1390000000-5eb2470575d7a40b35dd
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-0390000000-d91f1c70da42e9043a7b

Taxonomy

Description
This compound belongs to the class of organic compounds known as tryptamines and derivatives. These are compounds containing the tryptamine backbone, which is structurally characterized by an indole ring substituted at the 3-position by an ethanamine.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Indoles and derivatives
Sub Class
Tryptamines and derivatives
Direct Parent
Tryptamines and derivatives
Alternative Parents
3-alkylindoles / Aralkylamines / Substituted pyrroles / Oxazolidinones / Benzenoids / Heteroaromatic compounds / Carbamate esters / Trialkylamines / Organic carbonic acids and derivatives / Oxacyclic compounds
show 5 more
Substituents
Tryptamine / 3-alkylindole / Indole / Aralkylamine / Oxazolidinone / Substituted pyrrole / Benzenoid / Oxazolidine / Pyrrole / Heteroaromatic compound
show 16 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
tryptamines (CHEBI:10124)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. Le Grand B, Panissie A, Perez M, Pauwels PJ, John GW: Zolmitriptan stimulates a Ca(2+)-dependent K(+) current in C6 glioma cells stably expressing recombinant human 5-HT(1B) receptors. Eur J Pharmacol. 2000 Jun 2;397(2-3):297-302. [PubMed:10844127]
  2. Johnson DE, Rollema H, Schmidt AW, McHarg AD: Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001 Aug 17;425(3):203-10. [PubMed:11513839]
  3. de Almeida RM, Nikulina EM, Faccidomo S, Fish EW, Miczek KA: Zolmitriptan--a 5-HT1B/D agonist, alcohol, and aggression in mice. Psychopharmacology (Berl). 2001 Sep;157(2):131-41. [PubMed:11594437]
  4. Reuter U, Salomone S, Ickenstein GW, Waeber C: Effects of chronic sumatriptan and zolmitriptan treatment on 5-HT receptor expression and function in rats. Cephalalgia. 2004 May;24(5):398-407. [PubMed:15096229]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  6. Whale R, Bhagwagar Z, Cowen PJ: Zolmitriptan-induced growth hormone release in humans: mediation by 5-HT1D receptors? Psychopharmacology (Berl). 1999 Jul;145(2):223-6. [PubMed:10463324]
  7. Hargreaves RJ, Shepheard SL: Pathophysiology of migraine--new insights. Can J Neurol Sci. 1999 Nov;26 Suppl 3:S12-9. [PubMed:10563228]
  8. Gowin JL, Swann AC, Moeller FG, Lane SD: Zolmitriptan and human aggression: interaction with alcohol. Psychopharmacology (Berl). 2010 Jul;210(4):521-31. doi: 10.1007/s00213-010-1851-6. Epub 2010 Apr 21. [PubMed:20407761]
  9. Pascual J: [Mechanism of action of zolmitriptan]. Neurologia. 1998 Oct;13 Suppl 2:9-15. [PubMed:9859690]
  10. Martin GR: Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine. Cephalalgia. 1997 Oct;17 Suppl 18:4-14. [PubMed:9399012]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. Whale R, Bhagwagar Z, Cowen PJ: Zolmitriptan-induced growth hormone release in humans: mediation by 5-HT1D receptors? Psychopharmacology (Berl). 1999 Jul;145(2):223-6. [PubMed:10463324]
  2. Hargreaves RJ, Shepheard SL: Pathophysiology of migraine--new insights. Can J Neurol Sci. 1999 Nov;26 Suppl 3:S12-9. [PubMed:10563228]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  4. Le Grand B, Panissie A, Perez M, Pauwels PJ, John GW: Zolmitriptan stimulates a Ca(2+)-dependent K(+) current in C6 glioma cells stably expressing recombinant human 5-HT(1B) receptors. Eur J Pharmacol. 2000 Jun 2;397(2-3):297-302. [PubMed:10844127]
  5. Johnson DE, Rollema H, Schmidt AW, McHarg AD: Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001 Aug 17;425(3):203-10. [PubMed:11513839]
  6. de Almeida RM, Nikulina EM, Faccidomo S, Fish EW, Miczek KA: Zolmitriptan--a 5-HT1B/D agonist, alcohol, and aggression in mice. Psychopharmacology (Berl). 2001 Sep;157(2):131-41. [PubMed:11594437]
  7. Reuter U, Salomone S, Ickenstein GW, Waeber C: Effects of chronic sumatriptan and zolmitriptan treatment on 5-HT receptor expression and function in rats. Cephalalgia. 2004 May;24(5):398-407. [PubMed:15096229]
  8. Gowin JL, Swann AC, Moeller FG, Lane SD: Zolmitriptan and human aggression: interaction with alcohol. Psychopharmacology (Berl). 2010 Jul;210(4):521-31. doi: 10.1007/s00213-010-1851-6. Epub 2010 Apr 21. [PubMed:20407761]
  9. Pascual J: [Mechanism of action of zolmitriptan]. Neurologia. 1998 Oct;13 Suppl 2:9-15. [PubMed:9859690]
  10. Martin GR: Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine. Cephalalgia. 1997 Oct;17 Suppl 18:4-14. [PubMed:9399012]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that trig...
Gene Name
HTR1F
Uniprot ID
P30939
Uniprot Name
5-hydroxytryptamine receptor 1F
Molecular Weight
41708.505 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Reuter U, Salomone S, Ickenstein GW, Waeber C: Effects of chronic sumatriptan and zolmitriptan treatment on 5-HT receptor expression and function in rats. Cephalalgia. 2004 May;24(5):398-407. [PubMed:15096229]
  3. Villalon CM, Centurion D, Valdivia LF, de Vries P, Saxena PR: Migraine: pathophysiology, pharmacology, treatment and future trends. Curr Vasc Pharmacol. 2003 Mar;1(1):71-84. [PubMed:15320857]
  4. Villalon CM, Centurion D, Valdivia LF, De Vries P, Saxena PR: An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210. [PubMed:12434581]
  5. Bhalla P, Sharma HS, Wurch T, Pauwels PJ, Saxena PR: Molecular cloning and expression of the porcine trigeminal ganglion cDNA encoding a 5-ht(1F) receptor. Eur J Pharmacol. 2002 Feb 1;436(1-2):23-33. [PubMed:11834243]
  6. Wainscott DB, Johnson KW, Phebus LA, Schaus JM, Nelson DL: Human 5-HT1F receptor-stimulated [35S]GTPgammaS binding: correlation with inhibition of guinea pig dural plasma protein extravasation. Eur J Pharmacol. 1998 Jul 3;352(1):117-24. [PubMed:9718276]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Johnson DE, Rollema H, Schmidt AW, McHarg AD: Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001 Aug 17;425(3):203-10. [PubMed:11513839]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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 oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Yu LS, Yao TW, Zeng S: In vitro metabolism of zolmitriptan in rat cytochromes induced with beta-naphthoflavone and the interaction between six drugs and zolmitriptan. Chem Biol Interact. 2003 Dec 15;146(3):263-72. [PubMed:14642738]
  2. Wild MJ, McKillop D, Butters CJ: Determination of the human cytochrome P450 isoforms involved in the metabolism of zolmitriptan. Xenobiotica. 1999 Aug;29(8):847-57. [PubMed:10553725]
  3. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Serotonin binding
Specific Function
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...
Gene Name
MAOA
Uniprot ID
P21397
Uniprot Name
Amine oxidase [flavin-containing] A
Molecular Weight
59681.27 Da
References
  1. Rolan P: Potential drug interactions with the novel antimigraine compound zolmitriptan (Zomig, 311C90). Cephalalgia. 1997 Oct;17 Suppl 18:21-7. [PubMed:9399014]
  2. Wild MJ, McKillop D, Butters CJ: Determination of the human cytochrome P450 isoforms involved in the metabolism of zolmitriptan. Xenobiotica. 1999 Aug;29(8):847-57. [PubMed:10553725]
  3. Med-Psych Interactions Review: Triptans [File]

Drug created on June 13, 2005 07:24 / Updated on November 13, 2019 18:22