You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameEletriptan
Accession NumberDB00216  (APRD00945)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Eletriptan is a second generation triptan drug developed by Pfizer Inc for the treatment of migraine headaches. [Wikipedia]

Structure
Thumb
Synonyms
Eletriptanum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Gd-eletriptantablet20 mgoralGenmed A Division Of Pfizer Canada Inc2012-10-11Not applicableCanada
Gd-eletriptantablet40 mgoralGenmed A Division Of Pfizer Canada Inc2012-10-11Not applicableCanada
PMS-eletriptantablet40 mgoralPharmascience Inc2014-11-26Not applicableCanada
PMS-eletriptantablet20 mgoralPharmascience Inc2014-11-26Not applicableCanada
Relpaxtablet, film coated20 mg/1oralRoerig2002-12-26Not applicableUs
Relpaxtablet40 mgoralPfizer Canada Inc2004-10-13Not applicableCanada
Relpaxtablet20 mgoralPfizer Canada Inc2004-10-13Not applicableCanada
Relpaxtablet, film coated40 mg/1oralU.S. Pharmaceuticals2002-12-26Not applicableUs
Relpaxtablet, film coated40 mg/1oralPhysicians Total Care, Inc.2007-11-19Not applicableUs
Relpaxtablet, film coated40 mg/1oralRebel Distributors Corp2002-12-26Not applicableUs
Relpaxtablet, film coated40 mg/1oralSTAT Rx USA LLC2002-12-26Not applicableUs
Relpaxtablet, film coated40 mg/1oralRoerig2002-12-26Not applicableUs
Teva-eletriptantablet40 mgoralTeva Canada Limited2013-12-20Not applicableCanada
Teva-eletriptantablet20 mgoralTeva Canada Limited2013-12-20Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-eletriptantablet20 mgoralApotex Inc2013-09-12Not applicableCanada
Apo-eletriptantablet40 mgoralApotex Inc2013-09-12Not applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Eletriptan hydrobromide
ThumbNot applicableDBSALT000884
Categories
UNII22QOO9B8KI
CAS number143322-58-1
WeightAverage: 382.519
Monoisotopic: 382.171498776
Chemical FormulaC22H26N2O2S
InChI KeyInChIKey=PWVXXGRKLHYWKM-LJQANCHMSA-N
InChI
InChI=1S/C22H26N2O2S/c1-24-12-5-6-19(24)15-18-16-23-22-10-9-17(14-21(18)22)11-13-27(25,26)20-7-3-2-4-8-20/h2-4,7-10,14,16,19,23H,5-6,11-13,15H2,1H3/t19-/m1/s1
IUPAC Name
5-[2-(benzenesulfonyl)ethyl]-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-1H-indole
SMILES
CN1CCC[C@@H]1CC1=CNC2=C1C=C(CCS(=O)(=O)C1=CC=CC=C1)C=C2
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as indoles. These are compounds containing an indole moiety, which consists of pyrrole ring fused to benzene to form 2,3-benzopyrrole.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassIndoles
Direct ParentIndoles
Alternative Parents
Substituents
  • Indole
  • Aralkylamine
  • Benzenoid
  • N-alkylpyrrolidine
  • Substituted pyrrole
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Sulfonyl
  • Sulfone
  • Pyrrolidine
  • Pyrrole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the acute treatment of migraine with or without aura in adults.
PharmacodynamicsEletriptan is a selective 5-hydroxytryptamine 1B/1D receptor agonist. In the anesthetized dog, eletriptan has been shown to reduce carotid arterial blood flow, with only a small increase in arterial blood pressure at high doses. While the effect on blood flow was selective for the carotid arterial bed, decreases in coronary artery diameter were observed. Eletriptan has also been shown to inhibit trigeminal nerve activity in the rat.
Mechanism of actionEletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors, and little or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT6 receptors. Eletriptan has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors. Two theories have been proposed to explain the efficacy of 5-HT receptor agonists in migraine. One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of migraine headache. The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.
Related Articles
AbsorptionWell absorbed after oral administration with a mean absolute bioavailability of approximately 50%.
Volume of distribution
  • 138 L
Protein bindingPlasma protein binding is moderate and approximately 85%.
Metabolism

In vitro studies indicate that eletriptan is primarily metabolized by cytochrome P-450 enzyme CYP3A4. The N-demethylated metabolite of eletriptan is the only known active metabolite.

SubstrateEnzymesProduct
Eletriptan
N-DesmethyleletriptanDetails
Eletriptan
Eletriptan N-oxideDetails
Route of eliminationNot Available
Half lifeThe terminal elimination half-life of eletriptan is approximately 4 hours.
Clearance
  • Renal cl=3.9 L/h
ToxicityBased on the pharmacology of the 5-HT1B/1D agonists, hypertension or other more serious cardiovascular symptoms could occur on overdose.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3
Gene symbol: GNB3
UniProt: P16520
rs5443 Not AvailableT AlleleBetter response to drug treatment17361120
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9872
Blood Brain Barrier+0.9774
Caco-2 permeable-0.628
P-glycoprotein substrateSubstrate0.6308
P-glycoprotein inhibitor INon-inhibitor0.8046
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterInhibitor0.7
CYP450 2C9 substrateNon-substrate0.6591
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.643
CYP450 1A2 substrateNon-inhibitor0.7021
CYP450 2C9 inhibitorNon-inhibitor0.8103
CYP450 2D6 inhibitorNon-inhibitor0.7615
CYP450 2C19 inhibitorNon-inhibitor0.7519
CYP450 3A4 inhibitorNon-inhibitor0.6355
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6986
Ames testNon AMES toxic0.5945
CarcinogenicityNon-carcinogens0.8556
BiodegradationNot ready biodegradable0.9883
Rat acute toxicity2.5492 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6436
hERG inhibition (predictor II)Inhibitor0.7581
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Pfizer ireland pharmaceuticals
Packagers
Dosage forms
FormRouteStrength
Tabletoral20 mg
Tabletoral40 mg
Tablet, film coatedoral20 mg/1
Tablet, film coatedoral40 mg/1
Prices
Unit descriptionCostUnit
Relpax 6 20 mg tablet Box156.05USD box
Relpax 6 40 mg tablet Box156.05USD box
Relpax 20 mg tablet25.01USD tablet
Relpax 40 mg tablet25.01USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2198599 No2000-06-062015-05-17Canada
CA2352392 No2006-01-242019-11-01Canada
US5545644 No1996-12-262016-12-26Us
US6110940 No1997-08-292017-08-29Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityReadily soluble as hydrobromide formulationNot Available
logP3.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00118 mg/mLALOGPS
logP3.84ALOGPS
logP3.77ChemAxon
logS-5.5ALOGPS
pKa (Strongest Acidic)17.11ChemAxon
pKa (Strongest Basic)8.37ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area53.17 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity110.94 m3·mol-1ChemAxon
Polarizability42.99 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
References
Synthesis Reference

Ronald Ogilvie, “Process for the preparation of eletriptan.” U.S. Patent US20050059828, issued March 17, 2005.

US20050059828
General ReferencesNot Available
External Links
ATC CodesN02CC06
AHFS Codes
  • 28:32.28
PDB EntriesNot Available
FDA labelDownload (148 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcepromazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Acetophenazine.
AmisulprideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Amisulpride.
AprepitantThe serum concentration of Eletriptan can be increased when it is combined with Aprepitant.
AripiprazoleThe risk or severity of adverse effects can be increased when Eletriptan is combined with Aripiprazole.
AtazanavirThe serum concentration of Eletriptan can be increased when it is combined with Atazanavir.
BenzquinamideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Benzquinamide.
BoceprevirThe serum concentration of Eletriptan can be increased when it is combined with Boceprevir.
BromocriptineBromocriptine may increase the vasoconstricting activities of Eletriptan.
CabergolineCabergoline may increase the vasoconstricting activities of Eletriptan.
CarphenazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Carphenazine.
CeritinibThe serum concentration of Eletriptan can be increased when it is combined with Ceritinib.
ChlormezanoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Chlorprothixene.
ClarithromycinThe serum concentration of Eletriptan can be increased when it is combined with Clarithromycin.
ClozapineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Clozapine.
CobicistatThe serum concentration of Eletriptan can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Eletriptan can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Eletriptan can be increased when it is combined with Crizotinib.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Eletriptan.
DarunavirThe serum concentration of Eletriptan can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Eletriptan can be increased when it is combined with Dasatinib.
DelavirdineThe serum concentration of Eletriptan can be increased when it is combined with Delavirdine.
DihydroergotamineDihydroergotamine may increase the vasoconstricting activities of Eletriptan.
DiltiazemThe serum concentration of Eletriptan can be increased when it is combined with Diltiazem.
DronedaroneThe serum concentration of Eletriptan can be increased when it is combined with Dronedarone.
DroperidolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Droperidol.
DroxidopaEletriptan may increase the hypertensive activities of Droxidopa.
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Eletriptan.
ErgonovineErgonovine may increase the vasoconstricting activities of Eletriptan.
ErgotamineErgotamine may increase the vasoconstricting activities of Eletriptan.
ErythromycinThe serum concentration of Eletriptan can be increased when it is combined with Erythromycin.
FencamfamineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Fencamfamine.
FluconazoleThe serum concentration of Eletriptan can be increased when it is combined with Fluconazole.
FlupentixolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Fluspirilene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Eletriptan.
FosamprenavirThe serum concentration of Eletriptan can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Eletriptan can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Eletriptan can be increased when it is combined with Fusidic Acid.
GranisetronGranisetron may increase the serotonergic activities of Eletriptan.
HaloperidolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Haloperidol.
IdelalisibThe serum concentration of Eletriptan can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Eletriptan can be increased when it is combined with Imatinib.
IndinavirThe serum concentration of Eletriptan can be increased when it is combined with Indinavir.
IsavuconazoniumThe serum concentration of Eletriptan can be increased when it is combined with Isavuconazonium.
ItraconazoleThe serum concentration of Eletriptan can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Eletriptan can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Eletriptan can be increased when it is combined with Ketoconazole.
LoxapineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Loxapine.
LuliconazoleThe serum concentration of Eletriptan can be increased when it is combined with Luliconazole.
MesoridazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Mesoridazine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Methotrimeprazine.
MetoclopramideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Metoclopramide.
MifepristoneThe serum concentration of Eletriptan can be increased when it is combined with Mifepristone.
MolindoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Molindone.
NefazodoneThe serum concentration of Eletriptan can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Eletriptan can be increased when it is combined with Nelfinavir.
NilotinibThe serum concentration of Eletriptan can be increased when it is combined with Nilotinib.
OlanzapineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Eletriptan is combined with Ondansetron.
PalbociclibThe serum concentration of Eletriptan can be increased when it is combined with Palbociclib.
PaliperidoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Paliperidone.
PerphenazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Perphenazine.
PimozideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Piperacetazine.
PosaconazoleThe serum concentration of Eletriptan can be increased when it is combined with Posaconazole.
ProchlorperazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Quetiapine.
RemoxiprideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Risperidone.
RitonavirThe serum concentration of Eletriptan can be increased when it is combined with Ritonavir.
SaquinavirThe serum concentration of Eletriptan can be increased when it is combined with Saquinavir.
SertindoleThe risk or severity of adverse effects can be increased when Eletriptan is combined with Sertindole.
SimeprevirThe serum concentration of Eletriptan can be increased when it is combined with Simeprevir.
StiripentolThe serum concentration of Eletriptan can be increased when it is combined with Stiripentol.
SulpirideThe risk or severity of adverse effects can be increased when Eletriptan is combined with Sulpiride.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Eletriptan.
TelaprevirThe serum concentration of Eletriptan can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Eletriptan can be increased when it is combined with Telithromycin.
ThioridazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Thiothixene.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Eletriptan.
TrifluoperazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Eletriptan is combined with Triflupromazine.
VerapamilThe serum concentration of Eletriptan can be increased when it is combined with Verapamil.
VoriconazoleThe serum concentration of Eletriptan can be increased when it is combined with Voriconazole.
ZiprasidoneThe risk or severity of adverse effects can be increased when Eletriptan is combined with Ziprasidone.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Eletriptan is combined with Zuclopenthixol.
Food Interactions
  • Exposure to the product (area below curve) and maximum concentrations are increased when product is taken with a high-fat meal.

Targets

Kind
Protein
Organism
Human
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 substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate c...
Gene Name:
HTR1D
Uniprot ID:
P28221
Molecular Weight:
41906.38 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. Napier C, Stewart M, Melrose H, Hopkins B, McHarg A, Wallis R: Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68. [PubMed:10193663 ]
  3. Wackenfors A, Jarvius M, Ingemansson R, Edvinsson L, Malmsjo M: Triptans induce vasoconstriction of human arteries and veins from the thoracic wall. J Cardiovasc Pharmacol. 2005 May;45(5):476-84. [PubMed:15821444 ]
  4. 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 ]
  5. Strijbos PJ, Parsons AA, Fugelli A: Eletriptan Pfizer. Curr Opin Investig Drugs. 2002 Sep;3(9):1359-68. [PubMed:12498013 ]
  6. Tfelt-Hansen P, De Vries P, Saxena PR: Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs. 2000 Dec;60(6):1259-87. [PubMed:11152011 ]
Kind
Protein
Organism
Human
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 substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
Molecular Weight:
43567.535 Da
References
  1. Napier C, Stewart M, Melrose H, Hopkins B, McHarg A, Wallis R: Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68. [PubMed:10193663 ]
  2. van den Broek RW, MaassenVanDenBrink A, de Vries R, Bogers AJ, Stegmann AP, Avezaat CJ, Saxena PR: Pharmacological analysis of contractile effects of eletriptan and sumatriptan on human isolated blood vessels. Eur J Pharmacol. 2000 Oct 27;407(1-2):165-73. [PubMed:11050304 ]
  3. Knyihar-Csillik E, Tajti J, Csillik AE, Chadaide Z, Mihaly A, Vecsei L: Effects of eletriptan on the peptidergic innervation of the cerebral dura mater and trigeminal ganglion, and on the expression of c-fos and c-jun in the trigeminal complex of the rat in an experimental migraine model. Eur J Neurosci. 2000 Nov;12(11):3991-4002. [PubMed:11069595 ]
  4. 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 ]
  5. Lambert GA, Boers PM, Hoskin KL, Donaldson C, Zagami AS: Suppression by eletriptan of the activation of trigeminovascular sensory neurons by glyceryl trinitrate. Brain Res. 2002 Oct 25;953(1-2):181-8. [PubMed:12384251 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
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 triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity.
Gene Name:
HTR1F
Uniprot ID:
P30939
Molecular Weight:
41708.505 Da
References
  1. Napier C, Stewart M, Melrose H, Hopkins B, McHarg A, Wallis R: Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68. [PubMed:10193663 ]
  2. 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 ]
  3. Jahnichen S, Radtke OA, Pertz HH: Involvement of 5-HT1B receptors in triptan-induced contractile responses in guinea-pig isolated iliac artery. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):54-63. Epub 2004 Jun 8. [PubMed:15185063 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity.
Gene Name:
HTR1E
Uniprot ID:
P28566
Molecular Weight:
41681.57 Da
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:17139284 ]
  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:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins ...
Gene Name:
HTR2B
Uniprot ID:
P41595
Molecular Weight:
54297.41 Da
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:17139284 ]
  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:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
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:17139284 ]
  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:17016423 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
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.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da
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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Evans DC, O'Connor D, Lake BG, Evers R, Allen C, Hargreaves R: Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein. Drug Metab Dispos. 2003 Jul;31(7):861-9. [PubMed:12814962 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on June 30, 2016 01:50