Drugbank Logo

Showing drug card for Sumatriptan (DB00669)

Legend: drug field target field enzyme field

for drugs
Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-04-16 16:47:53
Primary Accession Number DB00669
Secondary Accession Number
  • APRD00379
Name Sumatriptan
Drug Type
  • Approved
  • Investigational
  • Small Molecule
Description A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of migraine disorders. A transdermal patch version of sumatriptan is currently in phase I trials in the U.S. under the code name NP101 (NuPathe).
Synonyms
  1. NP101
  2. Sumatriptan Succinate
  3. Sumatriptanum [INN-Latin]
  4. estradiol
  5. sumatriptan
  6. triptan
Brand Names
  1. Imigran
  2. Imitrex
  3. Sumatran
  4. Sumax
Brand Mixtures Not Available
Chemical IUPAC Name 1-[3-(2-dimethylaminoethyl)-1H-indol-5-yl]-N-methylmethanesulfonamide
Chemical Formula C14H21N3O2S
Chemical Structure Structure
CAS Registry Number 103628-46-2
InChI Identifier InChI=1/C14H21N3O2S/c1-15-20(18,19)10-11-4-5-14-13(8-11)12(9-16-14)6-7-17(2)3/h4-5,8-9,15-16H,6-7,10H2,1-3H3
InChI Key KQKPFRSPSRPDEB-UHFFFAOYAF
KEGG Drug D00451 Link Image
KEGG Compound C07319 Link Image
PubChem Compound 5358 Link Image
PubChem Substance 7847517 Link Image
ChEBI ID 10650 Link Image
PharmGKB ID PA451566 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02239738 Link Image
RxList Link http://www.rxlist.com/cgi/generic/sumitr.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Sumatriptan Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference M. D. Dowle, I. H. Coates, U.S. Pat. 4,816,470 (1989)
Average Molecular Weight 295.4000
Monoisotopic Molecular Weight 295.1354
State Solid
Melting Point 169-171 oC
Experimental Water Solubility 21.4 mg/ml Source: PhysProp
Predicted Water Solubility 1.27e-01 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 0.8 Source: PhysProp
Predicted LogP 1.17 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -3.37 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES CNS(=O)(=O)CC1=CC2=C(NC=C2CCN(C)C)C=C1
Canonical SMILES CNS(=O)(=O)CC1=CC2=C(NC=C2CCN(C)C)C=C1
Drug Category
  • Selective Serotonin Agonists
  • Serotonin Agonists
  • Vasoconstrictor Agents
ATC Codes
AHFS Codes
  • 28:32.28
Indication For the treatment of migraine attacks with or without aura in adults
Pharmacology Sumatriptan, an antimigraine drug, is structurally similar to serotonin. It is thought that the cerebral blood vessel constriction induced by activation of 5-HT1 receptors on those vessels may contribute to the antimigrainous effect of sumatriptan in humans.
Mechanism of Action Sumatriptan stimulates 5-HT receptors of the 1D subtype, most likely presynaptic receptors, resulting in selective vasoconstriction of inflamed and dilated cranial blood vessels in the carotid circulation. Sumatriptan also blocks the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater during migraine and may inhibit the release of inflammatory mediators from the trigeminal nerve.
Absorption Approximately 15%
Toxicity Symptoms of overdose include convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation.
Protein Binding 14%-21%
Biotransformation Hepatic. In vitro studies with human microsomes suggest that sumatriptan is metabolized by monoamine oxidase (MAO), predominantly the A isoenzyme.
Half Life 2.5 hours
Dosage Forms
Form Route
Liquid Subcutaneous
Patch, extended release Transdermal
Spray Nasal
Tablet Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. Drugs.com Link Image
  2. Wikipedia Link Image
  3. RxList Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Monoamine oxidase type A (MAO-A)
Targets
  1. 5-hydroxytryptamine 2B receptor
  2. 5-hydroxytryptamine 1F receptor
  3. 5-hydroxytryptamine 1D receptor
  4. 5-hydroxytryptamine 1B receptor
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Monoamine oxidase type A (MAO-A)
Enzyme 1 Gene Name MAOA
Enzyme 1 SwissProt ID P21397 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P21397|AOFA_HUMAN Amine oxidase [flavin-containing] 
MENQEKASIAGHMFDVVVIGGGISGLSAAKLLTEYGVSVLVLEARDRVGGRTYTIRNEHV
DYVDVGGAYVGPTQNRILRLSKELGIETYKVNVSERLVQYVKGKTYPFRGAFPPVWNPIA
YLDYNNLWRTIDNMGKEIPTDAPWEAQHADKWDKMTMKELIDKICWTKTARRFAYLFVNI
NVTSEPHEVSALWFLWYVKQCGGTTRIFSVTNGGQERKFVGGSGQVSERIMDLLGDQVKL
NHPVTHVDQSSDNIIIETLNHEHYECKYVINAIPPTLTAKIHFRPELPAERNQLIQRLPM
GAVIKCMMYYKEAFWKKKDYCGCMIIEDEDAPISITLDDTKPDGSLPAIMGFILARKADR
LAKLHKEIRKKKICELYAKVLGSQEALHPVHYEEKNWCEEQYSGGCYTAYFPPGIMTQYG
RVIRQPVGRIFFAGTETATKWSGYMEGAVEAGERAAREVLNGLGKVTEKDIWVQEPESKD
VPAVEITHTFWERNLPSVSGLLKIIGFSTSVTALGFVLYKYKLLPRS
Drug Target 1 [top]
Target 1 ID 436
Target 1 Name 5-hydroxytryptamine 2B receptor
Target 1 Synonyms
  1. 5-HT-2B
  2. Serotonin receptor 2B
Target 1 Gene Name HTR2B
Target 1 Protein Sequence >5-hydroxytryptamine 2B receptor 
MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALL
ILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAM
WPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVW
LISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLT
IHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDET
LMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQM
LLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNP
MAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSY
V
Target 1 Number of Residues 489
Target 1 Molecular Weight 54299
Target 1 Theoretical pI 9.47
Target 1 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in rhodopsin-like receptor activity
Target 1 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. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 57-79
  • 92-113
  • 130-151
  • 172-192
  • 217-239
  • 325-345
  • 361-383
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 475198 Link Image
Target 1 UniProtKB/Swiss-Prot ID P41595 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name 5HT2B_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >1446 bp 
ATGGCTCTCTCTTACAGAGTGTCTGAACTTCAAAGCACAATTCCTGAGCACATTTTGCAG
AGCACCTTTGTTCACGTTATCTCTTCTAACTGGTCTGGATTACAGACAGAATCAATACCA
GAGGAAATGAAACAGATTGTTGAGGAACAGGGAAATAAACTGCACTGGGCAGCTCTTCTG
ATACTCATGGTGATAATACCCACAATTGGTGGAAATACCCTTGTTATTCTGGCTGTTTCA
CTGGAGAAGAAGCTGCAGTATGCTACTAATTACTTTCTAATGTCCTTGGCGGTGGCTGAT
TTGCTGGTTGGATTGTTTGTGATGCCAATTGCCCTCTTGACAATAATGTTTGAGGCTATG
TGGCCCCTCCCACTTGTTCTATGTCCTGCCTGGTTATTTCTTGACGTTCTCTTTTCAACC
GCATCCATCATGCATCTCTGTGCCATTTCAGTGGATCGTTACATAGCCATCAAAAAGCCA
ATCCAGGCCAATCAATATAACTCACGGGCTACAGCATTCATCAAGATTACAGTGGTGTGG
TTAATTTCAATAGGCATTGCCATTCCAGTCCCTATTAAAGGGATAGAGACTGATGTGGAC
AACCCAAACAATATCACTTGTGTGCTGACAAAGGAACGTTTTGGCGATTTCATGCTCTTT
GGCTCACTGGCTGCCTTCTTCACACCTCTTGCAATTATGATTGTCACCTACTTTCTCACT
ATCCATGCTTTACAGAAGAAGGCTTACTTAGTCAAAAACAAGCCACCTCAACGCCTAACA
TGGTTGACTGTGTCTACAGTTTTCCAAAGGGATGAAACACCTTGCTCGTCACCGGAAAAG
GTGGCAATGCTGGATGGTTCTCGAAAGGACAAGGCTCTGCCCAACTCAGGTGATGAAACA
CTTATGCGAAGAACATCCACAATTGGGAAAAAGTCAGTGCAGACCATTTCCAACGAACAG
AGAGCCTCAAAGGTCCTAGGGATTGTGTTTTTCCTCTTTTTGCTTATGTGGTGTCCCTTC
TTTATTACAAATATAACTTTAGTTTTATGTGATTCCTGTAACCAAACTACTCTCCAAATG
CTCCTGGAGATATTTGTGTGGATAGGCTATGTTTCCTCAGGAGTGAATCCTTTGGTCTAC
ACCCTCTTCAATAAGACATTTCGGGATGCATTTGGCCGATATATCACCTGCAATTACCGG
GCCACAAAGTCAGTAAAAACTCTCAGAAAACGCTCCAGTAAGATCTACTTCCGGAATCCA
ATGGCAGAGAACTCTAAGTTTTTCAAGAAACATGGAATTCGAAATGGGATTAACCCTGCC
ATGTACCAGAGTCCAATGAGGCTCCGAAGTTCAACCATTCAGTCTTCATCAATCATTCTA
CTAGATACGCTTCTCCTCACTGAAAATGAAGGTGACAAAACTGAAGAGCAAGTTAGTTAT
GTATAG
Target 1 GenBank Gene ID
Target 1 GeneCard ID HTR2B Link Image
Target 1 GenAtlas ID HTR2B Link Image
Target 1 HGNC ID HGNC:5294 Link Image
Target 1 Chromosome Location 2
Target 1 Locus 2q36.3-q37.1
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Kim SJ, Veenstra-VanderWeele J, Hanna GL, Gonen D, Leventhal BL, Cook EH Jr: Mutation screening of human 5-HT(2B)receptor gene in early-onset obsessive-compulsive disorder. Mol Cell Probes. 2000 Feb;14(1):47-52. [PubMed Link Image]
  2. Becamel C, Figge A, Poliak S, Dumuis A, Peles E, Bockaert J, Lubbert H, Ullmer C: Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1. J Biol Chem. 2001 Apr 20;276(16):12974-82. Epub 2001 Jan 9. [PubMed Link Image]
  3. Choi DS, Birraux G, Launay JM, Maroteaux L: The human serotonin 5-HT2B receptor: pharmacological link between 5-HT2 and 5-HT1D receptors. FEBS Lett. 1994 Oct 3;352(3):393-9. [PubMed Link Image]
  4. Kursar JD, Nelson DL, Wainscott DB, Baez M: Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor. Mol Pharmacol. 1994 Aug;46(2):227-34. [PubMed Link Image]
  5. Schmuck K, Ullmer C, Engels P, Lubbert H: Cloning and functional characterization of the human 5-HT2B serotonin receptor. FEBS Lett. 1994 Mar 28;342(1):85-90. [PubMed Link Image]
Target 1 Drug References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 511
Target 2 Name 5-hydroxytryptamine 1F receptor
Target 2 Synonyms
  1. 5-HT-1F
  2. Serotonin receptor 1F
Target 2 Gene Name HTR1F
Target 2 Protein Sequence >5-hydroxytryptamine 1F receptor 
MDFLNSSDQNLTSEELLNRMPSKILVSLTLSGLALMTTTINSLVIAAIIVTRKLHHPANY
LICSLAVTDFLVAVLVMPFSIVYIVRESWIMGQVVCDIWLSVDITCCTCSILHLSAIALD
RYRAITDAVEYARKRTPKHAGIMITIVWIISVFISMPPLFWRHQGTSRDDECIIKHDHIV
STIYSTFGAFYIPLALILILYYKIYRAAKTLYHKRQASRIAKEEVNGQVLLESGEKSTKS
VSTSYVLEKSLSDPSTDFDKIHSTVRSLRSEFKHEKSWRRQKISGTRERKAATTLGLILG
AFVICWLPFFVKELVVNVCDKCKISEEMSNFLAWLGYLNSLINPLIYTIFNEDFKKAFQK
LVRCRC
Target 2 Number of Residues 372
Target 2 Molecular Weight 41709
Target 2 Theoretical pI 9.08
Target 2 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Involved in rhodopsin-like receptor activity
Target 2 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 inhibit adenylate cyclase activity
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 24-48
  • 61-83
  • 95-119
  • 140-161
  • 179-202
  • 292-314
  • 328-351
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 307420 Link Image
Target 2 UniProtKB/Swiss-Prot ID P30939 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name 5HT1F_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 2 Gene Sequence >1101 bp 
ATGGATTTCTTAAATTCATCTGATCAAAACTTGACCTCAGAGGAACTGTTAAACAGAATG
CCATCCAAAATTCTGGTGTCCCTCACTCTGTCTGGGCTGGCACTGATGACAACAACTATC
AACTCCCTTGTGATCGCTGCAATTATTGTGACCCGGAAGCTGCACCATCCAGCCAATTAT
TTAATTTGTTCCCTTGCAGTCACAGATTTTCTTGTGGCTGTCCTGGTGATGCCCTTCAGC
ATTGTGTATATTGTGAGAGAGAGCTGGATTATGGGGCAAGTGGTCTGTGACATTTGGCTG
AGTGTTGACATTACCTGCTGCACGTGCTCCATCTTGCATCTCTCAGCTATAGCTTTGGAT
CGGTATCGAGCAATCACAGATGCTGTTGAGTATGCCAGGAAAAGGACTCCAAAGCATGCT
GGCATTATGATTACAATAGTTTGGATTATATCTGTTTTTATCTCTATGCCTCCTCTATTC
TGGAGGCACCAAGGAACTAGCAGAGATGATGAATGCATCATCAAGCACGACCACATTGTT
TCCACCATTTACTCAACATTTGGAGCTTTCTACATCCCACTGGCATTGATTTTGATCCTT
TACTACAAAATATATAGAGCAGCAAAGACATTATACCACAAGAGACAAGCAAGTAGGATT
GCAAAGGAGGAGGTGAATGGCCAAGTCCTTTTGGAGAGTGGTGAGAAAAGCACTAAATCA
GTTTCCACATCCTATGTACTAGAAAAGTCTTTATCTGACCCATCAACAGACTTTGATAAA
ATTCATAGCACAGTGAGAAGTCTCAGGTCTGAATTCAAGCATGAGAAATCTTGGAGAAGG
CAAAAGATCTCAGGTACAAGAGAACGGAAAGCAGCCACTACCCTGGGATTAATCTTGGGT
GCATTTGTAATATGTTGGCTTCCTTTTTTTGTAAAAGAATTAGTTGTTAATGTCTGTGAC
AAATGTAAAATTTCTGAAGAAATGTCCAATTTTTTGGCATGGCTTGGGTATCTCAATTCC
CTTATAAATCCACTGATTTACACAATCTTTAATGAAGACTTCAAGAAAGCATTCCAAAAG
CTTGTGCGATGTCGATGTTAG
Target 2 GenBank Gene ID
Target 2 GeneCard ID HTR1F Link Image
Target 2 GenAtlas ID HTR1F Link Image
Target 2 HGNC ID HGNC:5292 Link Image
Target 2 Chromosome Location 3
Target 2 Locus 3p12
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA: Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. Proc Natl Acad Sci U S A. 1993 Jan 15;90(2):408-12. [PubMed Link Image]
  2. Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG: Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes. Proc Natl Acad Sci U S A. 1993 Mar 15;90(6):2184-8. [PubMed Link Image]
Target 2 Drug References
  1. Razzaque Z, Heald MA, Pickard JD, Maskell L, Beer MS, Hill RG, Longmore J: Vasoconstriction in human isolated middle meningeal arteries: determining the contribution of 5-HT1B- and 5-HT1F-receptor activation. Br J Clin Pharmacol. 1999 Jan;47(1):75-82. [PubMed Link Image]
  2. Pauwels PJ, John GW: Present and future of 5-HT receptor agonists as antimigraine drugs. Clin Neuropharmacol. 1999 May-Jun;22(3):123-36. [PubMed Link Image]
  3. Roy A, Brand NJ, Yacoub MH: Expression of 5-hydroxytryptamine receptor subtype messenger RNA in interstitial cells from human heart valves. J Heart Valve Dis. 2000 Mar;9(2):256-60; discussion 260-1. [PubMed Link Image]
  4. Cohen ML, Schenck K: Contractile responses to sumatriptan and ergotamine in the rabbit saphenous vein: effect of selective 5-HT(1F) receptor agonists and PGF(2alpha). Br J Pharmacol. 2000 Oct;131(3):562-8. [PubMed Link Image]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  6. Janssen P, Tack J, Sifrim D, Meulemans AL, Lefebvre RA: Influence of 5-HT1 receptor agonists on feline stomach relaxation. Eur J Pharmacol. 2004 May 25;492(2-3):259-67. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 725
Target 3 Name 5-hydroxytryptamine 1D receptor
Target 3 Synonyms
  1. 5- HT-1D-alpha
  2. 5-HT-1D
  3. Serotonin receptor 1D
Target 3 Gene Name HTR1D
Target 3 Protein Sequence >5-hydroxytryptamine 1D receptor 
MSPLNQSAEGLPQEASNRSLNATETSEAWDPRTLQALKISLAVVLSVITLATVLSNAFVL
TTILLTRKLHTPANYLIGSLATTDLLVSILVMPISIAYTITHTWNFGQILCDIWLSSDIT
CCTASILHLCVIALDRYWAITDALEYSKRRTAGHAATMIAIVWAISICISIPPLFWRQAK
AQEEMSDCLVNTSQISYTIYSTCGAFYIPSVLLIILYGRIYRAARNRILNPPSLYGKRFT
TAHLITGSAGSSLCSLNSSLHEGHSHSAGSPLFFNHVKIKLADSALERKRISAARERKAT
KILGIILGAFIICWLPFFVVSLVLPICRDSCWIHPALFDFFTWLGYLNSLINPIIYTVFN
EEFRQAFQKIVPFRKAS
Target 3 Number of Residues 383
Target 3 Molecular Weight 41907
Target 3 Theoretical pI 8.85
Target 3 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 3 General Function Involved in rhodopsin-like receptor activity
Target 3 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 inhibit adenylate cyclase activity
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 39-62
  • 76-98
  • 109-134
  • 155-176
  • 195-218
  • 303-326
  • 336-360
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 177772 Link Image
Target 3 UniProtKB/Swiss-Prot ID P28221 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name 5HT1D_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 Gene Sequence >1134 bp 
ATGTCCCCACTGAACCAGTCAGCAGAAGGCCTTCCCCAGGAGGCCTCCAACAGATCCCTG
AATGCCACAGAAACCTCAGAGGCTTGGGATCCCAGGACCCTCCAGGCGCTCAAGATCTCC
CTTGCCGTGGTCCTTTCCGTCATCACACTGGCCACAGTCCTCTCCAATGCCTTTGTACTC
ACCACCATCTTACTCACCAGGAAGCTCCACACCCCTGCCAACTACCTGATTGGCTCCCTG
GCCACCACCGACCTCTTGGTTTCCATCTTGGTAATGCCCATCAGCATCGCCTATACCATC
ACCCACACCTGGAACTTTGGCCAAATCTTGTGTGACATCTGGCTGTCCTCTGACATCACG
TGCTGCACAGCCTCCATCCTGCATCTCTGTGTCATTGCTCTGGACAGGTACTGGGCAATC
ACAGATGCCCTGGAATACAGTAAACGCAGGACGGCTGGCCACGCGGCCACCATGATCGCC
ATTGTCTGGGCCATCTCCATCTGCATCTCCATCCCCCCGCTCTTCTGGCGGCAGGCCAAG
GCCCAGGAGGAGATGTCGGACTGTCTGGTGAACACCTCTCAGATCTCCTACACCATCTAC
TCCACCTGTGGGGCCTTCTACATTCCCTCGGTGTTGCTCATCATCCTATATGGCCGGATC
TACCGGGCTGCCCGGAACCGCATCCTGAATCCACCCTCACTCTATGGGAAGCGCTTCACC
ACGGCCCACCTCATCACAGGCTCTGCCGGGTCCTCGCTCTGCTCGCTCAACTCCAGCCTC
CATGAGGGGCACTCGCACTCGGCTGGCTCCCCTCTCTTTTTCAACCACGTGAAAATCAAG
CTTGCTGACAGTGCCCTGGAACGCAAGAGGATTTCTGCTGCTCGAGAAAGGAAAGCCACT
AAAATCCTGGGCATCATTCTGGGGGCCTTTATCATCTGCTGGCTGCCCTTCTTCGTGGTG
TCTCTGGTCCTCCCCATCTGCCGGGACTCCTGCTGGATCCACCCGGCGCTCTTTGACTTC
TTCACCTGGCTAGGCTATTTAAACTCCCTCATCAATCCAATAATCTACACTGTGTTTAAT
GAAGAGTTTCGGCAAGCTTTTCAGAAAATTGTCCCTTTCCGGAAGGCCTCCTAG
Target 3 GenBank Gene ID
Target 3 GeneCard ID HTR1D Link Image
Target 3 GenAtlas ID HTR1D Link Image
Target 3 HGNC ID HGNC:5289 Link Image
Target 3 Chromosome Location 1
Target 3 Locus 1p36.3-p34.3
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Cargill M, Altshuler D, Ireland J, Sklar P, Ardlie K, Patil N, Shaw N, Lane CR, Lim EP, Kalyanaraman N, Nemesh J, Ziaugra L, Friedland L, Rolfe A, Warrington J, Lipshutz R, Daley GQ, Lander ES: Characterization of single-nucleotide polymorphisms in coding regions of human genes. Nat Genet. 1999 Jul;22(3):231-8. [PubMed Link Image]
  2. Weinshank RL, Zgombick JM, Macchi MJ, Branchek TA, Hartig PR: Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta. Proc Natl Acad Sci U S A. 1992 Apr 15;89(8):3630-4. [PubMed Link Image]
  3. Hamblin MW, Metcalf MA: Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol Pharmacol. 1991 Aug;40(2):143-8. [PubMed Link Image]
Target 3 Drug References
  1. Koran LM, Pallanti S, Quercioli L: Sumatriptan, 5-HT(1D) receptors and obsessive-compulsive disorder. Eur Neuropsychopharmacol. 2001 Apr;11(2):169-72. [PubMed Link Image]
  2. Baxter LR Jr: Brain mediation of Anolis social dominance displays. III. Differential forebrain 3H-sumatriptan binding in dominant vs. submissive males. Brain Behav Evol. 2001 Apr;57(4):202-13. [PubMed Link Image]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  4. Razzaque Z, Pickard JD, Ma QP, Shaw D, Morrison K, Wang T, Longmore J: 5-HT1B-receptors and vascular reactivity in human isolated blood vessels: assessment of the potential craniovascular selectivity of sumatriptan. Br J Clin Pharmacol. 2002 Mar;53(3):266-74. [PubMed Link Image]
  5. Akin D, Gurdal H: Involvement of 5-HT1B and 5-HT1D receptors in sumatriptan mediated vasocontractile response in rabbit common carotid artery. Br J Pharmacol. 2002 May;136(2):177-82. [PubMed Link Image]
  6. Zohar J, Kennedy JL, Hollander E, Koran LM: Serotonin-1D hypothesis of obsessive-compulsive disorder: an update. J Clin Psychiatry. 2004;65 Suppl 14:18-21. [PubMed Link Image]
Drug Target 4 [top]
Target 4 ID 885
Target 4 Name 5-hydroxytryptamine 1B receptor
Target 4 Synonyms
  1. 5- HT1B
  2. 5-HT-1B
  3. 5-HT-1D-beta
  4. S12
  5. Serotonin 1D beta receptor
  6. Serotonin receptor 1B
Target 4 Gene Name HTR1B
Target 4 Protein Sequence >5-hydroxytryptamine 1B receptor 
MEEPGAQCAPPPPAGSETWVPQANLSSAPSQNCSAKDYIYQDSISLPWKVLLVMLLALIT
LATTLSNAFVIATVYRTRKLHTPANYLIASLAVTDLLVSILVMPISTMYTVTGRWTLGQV
VCDFWLSSDITCCTASILHLCVIALDRYWAITDAVEYSAKRTPKRAAVMIALVWVFSISI
SLPPFFWRQAKAEEEVSECVVNTDHILYTVYSTVGAFYFPTLLLIALYGRIYVEARSRIL
KQTPNRTGKRLTRAQLITDSPGSTSSVTSINSRVPDVPSESGSPVYVNQVKVRVSDALLE
KKKLMAARERKATKTLGIILGAFIVCWLPFFIISLVMPICKDACWFHLAIFDFFTWLGYL
NSLINPIIYTMSNEDFKQAFHKLIRFKCTS
Target 4 Number of Residues 396
Target 4 Molecular Weight 43568
Target 4 Theoretical pI 8.82
Target 4 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 4 General Function Involved in rhodopsin-like receptor activity
Target 4 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 inhibit adenylate cyclase activity
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • 50-73
  • 87-109
  • 120-145
  • 166-187
  • 206-229
  • 316-340
  • 348-373
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 219679 Link Image
Target 4 UniProtKB/Swiss-Prot ID P28222 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name 5HT1B_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 4 Gene Sequence >1173 bp 
ATGGAGGAACCGGGTGCTCAGTGCGCTCCACCGCCGCCCGCGGGCTCCGAGACCTGGGTT
CCTCAAGCCAACTTATCCTCTGCTCCCTCCCAAAACTGCAGCGCCAAGGACTACATTTAC
CAGGACTCCATCTCCCTACCCTGGAAAGTACTGCTGGTTATGCTATTGGCGCTCATCACC
TTGGCCACCACGCTCTCCAATGCCTTTGTGATTGCCACAGTGTACCGGACCCGGAAACTG
CACACCCCGGCTAACTACCTGATCGCCTCTCTGGCGGTCACCGACCTGCTTGTGTCCATC
CTGGTGATGCCCATCAGCACCATGTACACTGTCACCGGCCGCTGGACACTGGGCCAGGTG
GTCTGTGACTTCTGGCTGTCGTCGGACATCACTTGTTGCACTGCCTCCATCCTGCACCTC
TGTGTCATCGCCCTGGACCGCTACTGGGCCATCACGGACGCCGTGGAGTACTCAGCTAAA
AGGACTCCCAAGAGGGCGGCGGTCATGATCGCGCTGGTGTGGGTCTTCTCCATCTCTATC
TCGCTGCCGCCCTTCTTCTGGCGTCAGGCTAAGGCCGAAGAGGAGGTGTCGGAATGCGTG
GTGAACACCGACCACATCCTCTACACGGTCTACTCCACGGTGGGTGCTTTCTACTTCCCC
ACCCTGCTCCTCATCGCCCTCTATGGCCGCATCTACGTAGAAGCCCGCTCCCGGATTTTG
AAACAGACGCCCAACAGGACCGGCAAGCGCTTGACCCGAGCCCAGCTGATAACCGACTCC
CCCGGGTCCACGTCCTCGGTCACCTCTATTAACTCGCGGGTTCCCGACGTGCCCAGCGAA
TCCGGATCTCCTGTGTATGTGAACCAAGTCAAAGTGCGAGTCTCCGACGCCCTGCTGGAA
AAGAAGAAACTCATGGCCGCTAGGGAGCGCAAAGCCACCAAGACCCTAGGGATCATTTTG
GGAGCCTTTATTGTGTGTTGGCTACCCTTCTTCATCATCTCCCTAGTGATGCCTATCTGC
AAAGATGCCTGCTGGTTCCACCTAGCCATCTTTGACTTCTTCACATGGCTGGGCTATCTC
AACTCCCTCATCAACCCCATAATCTATACCATGTCCAATGAGGACTTTAAACAAGCATTC
CATAAACTGATACGTTTTAAGTGCACAAGTTGA
Target 4 GenBank Gene ID
Target 4 GeneCard ID HTR1B Link Image
Target 4 GenAtlas ID HTR1B Link Image
Target 4 HGNC ID HGNC:5287 Link Image
Target 4 Chromosome Location 6
Target 4 Locus 6q13
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Hamblin MW, Metcalf MA, McGuffin RW, Karpells S: Molecular cloning and functional characterization of a human 5-HT1B serotonin receptor: a homologue of the rat 5-HT1B receptor with 5-HT1D-like pharmacological specificity. Biochem Biophys Res Commun. 1992 Apr 30;184(2):752-9. [PubMed Link Image]
  2. Veldman SA, Bienkowski MJ: Cloning and pharmacological characterization of a novel human 5-hydroxytryptamine1D receptor subtype. Mol Pharmacol. 1992 Sep;42(3):439-44. [PubMed Link Image]
  3. Jin H, Oksenberg D, Ashkenazi A, Peroutka SJ, Duncan AM, Rozmahel R, Yang Y, Mengod G, Palacios JM, O'Dowd BF: Characterization of the human 5-hydroxytryptamine1B receptor. J Biol Chem. 1992 Mar 25;267(9):5735-8. [PubMed Link Image]
  4. Demchyshyn L, Sunahara RK, Miller K, Teitler M, Hoffman BJ, Kennedy JL, Seeman P, Van Tol HH, Niznik HB: A human serotonin 1D receptor variant (5HT1D beta) encoded by an intronless gene on chromosome 6. Proc Natl Acad Sci U S A. 1992 Jun 15;89(12):5522-6. [PubMed Link Image]
  5. Mungall AJ, Palmer SA, Sims SK, Edwards CA, Ashurst JL, Wilming L, Jones MC, Horton R, Hunt SE, Scott CE, Gilbert JG, Clamp ME, Bethel G, Milne S, Ainscough R, Almeida JP, Ambrose KD, Andrews TD, Ashwell RI, Babbage AK, Bagguley CL, Bailey J, Banerjee R, Barker DJ, Barlow KF, Bates K, Beare DM, Beasley H, Beasley O, Bird CP, Blakey S, Bray-Allen S, Brook J, Brown AJ, Brown JY, Burford DC, Burrill W, Burton J, Carder C, Carter NP, Chapman JC, Clark SY, Clark G, Clee CM, Clegg S, Cobley V, Collier RE, Collins JE, Colman LK, Corby NR, Coville GJ, Culley KM, Dhami P, Davies J, Dunn M, Earthrowl ME, Ellington AE, Evans KA, Faulkner L, Francis MD, Frankish A, Frankland J, French L, Garner P, Garnett J, Ghori MJ, Gilby LM, Gillson CJ, Glithero RJ, Grafham DV, Grant M, Gribble S, Griffiths C, Griffiths M, Hall R, Halls KS, Hammond S, Harley JL, Hart EA, Heath PD, Heathcott R, Holmes SJ, Howden PJ, Howe KL, Howell GR, Huckle E, Humphray SJ, Humphries MD, Hunt AR, Johnson CM, Joy AA, Kay M, Keenan SJ, Kimberley AM, King A, Laird GK, Langford C, Lawlor S, Leongamornlert DA, Leversha M, Lloyd CR, Lloyd DM, Loveland JE, Lovell J, Martin S, Mashreghi-Mohammadi M, Maslen GL, Matthews L, McCann OT, McLaren SJ, McLay K, McMurray A, Moore MJ, Mullikin JC, Niblett D, Nickerson T, Novik KL, Oliver K, Overton-Larty EK, Parker A, Patel R, Pearce AV, Peck AI, Phillimore B, Phillips S, Plumb RW, Porter KM, Ramsey Y, Ranby SA, Rice CM, Ross MT, Searle SM, Sehra HK, Sheridan E, Skuce CD, Smith S, Smith M, Spraggon L, Squares SL, Steward CA, Sycamore N, Tamlyn-Hall G, Tester J, Theaker AJ, Thomas DW, Thorpe A, Tracey A, Tromans A, Tubby B, Wall M, Wallis JM, West AP, White SS, Whitehead SL, Whittaker H, Wild A, Willey DJ, Wilmer TE, Wood JM, Wray PW, Wyatt JC, Young L, Younger RM, Bentley DR, Coulson A, Durbin R, Hubbard T, Sulston JE, Dunham I, Rogers J, Beck S: The DNA sequence and analysis of human chromosome 6. Nature. 2003 Oct 23;425(6960):805-11. [PubMed Link Image]
  6. Levy FO, Gudermann T, Perez-Reyes E, Birnbaumer M, Kaumann AJ, Birnbaumer L: Molecular cloning of a human serotonin receptor (S12) with a pharmacological profile resembling that of the 5-HT1D subtype. J Biol Chem. 1992 Apr 15;267(11):7553-62. [PubMed Link Image]
  7. Weinshank RL, Zgombick JM, Macchi MJ, Branchek TA, Hartig PR: Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta. Proc Natl Acad Sci U S A. 1992 Apr 15;89(8):3630-4. [PubMed Link Image]
  8. Mochizuki D, Yuyama Y, Tsujita R, Komaki H, Sagai H: Cloning and expression of the human 5-HT1B-type receptor gene. Biochem Biophys Res Commun. 1992 Jun 15;185(2):517-23. [PubMed Link Image]
  9. Nothen MM, Erdmann J, Shimron-Abarbanell D, Propping P: Identification of genetic variation in the human serotonin 1D beta receptor gene. Biochem Biophys Res Commun. 1994 Dec 15;205(2):1194-200. [PubMed Link Image]
  10. Ng GY, George SR, Zastawny RL, Caron M, Bouvier M, Dennis M, O'Dowd BF: Human serotonin1B receptor expression in Sf9 cells: phosphorylation, palmitoylation, and adenylyl cyclase inhibition. Biochemistry. 1993 Nov 2;32(43):11727-33. [PubMed Link Image]
Target 4 Drug References
  1. Dupuis DS, Perez M, Halazy S, Colpaert FC, Pauwels PJ: Magnitude of 5-HT1B and 5-HT1A receptor activation in guinea-pig and rat brain: evidence from sumatriptan dimer-mediated [35S]GTPgammaS binding responses. Brain Res Mol Brain Res. 1999 Apr 6;67(1):107-23. [PubMed Link Image]
  2. Mitsikostas DD, Sanchez del Rio M, Moskowitz MA, Waeber C: Both 5-HT1B and 5-HT1F receptors modulate c-fos expression within rat trigeminal nucleus caudalis. Eur J Pharmacol. 1999 Mar 26;369(3):271-7. [PubMed Link Image]
  3. Cohen ML, Schenck KW, Hemrick-Luecke SH: 5-Hydroxytryptamine(1A) receptor activation enhances norepinephrine release from nerves in the rabbit saphenous vein. J Pharmacol Exp Ther. 1999 Sep;290(3):1195-201. [PubMed Link Image]
  4. Cohen Z, Bouchelet I, Olivier A, Villemure JG, Ball R, Stanimirovic DB, Hamel E: Multiple microvascular and astroglial 5-hydroxytryptamine receptor subtypes in human brain: molecular and pharmacologic characterization. J Cereb Blood Flow Metab. 1999 Aug;19(8):908-17. [PubMed Link Image]
  5. Granas C, Larhammar D: Identification of an amino acid residue important for binding of methiothepin and sumatriptan to the human 5-HT(1B) receptor. Eur J Pharmacol. 1999 Sep 10;380(2-3):171-81. [PubMed Link Image]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.