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Showing toxin card for Ergotamine (T3D2460)

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Version 1.0
Creation Date 2009-07-03 21:06:25
Update Date 2010-06-10 15:40:43
Accession Number T3D2460
Name Ergotamine
Compound Type
  • Adrenergic alpha-Agonist
  • Analgesic, Non-Narcotic
  • Drug
  • Mycotoxin
  • Sympatholytic
  • Vasoconstrictor Agent
Description Ergotamine is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It is a secondary metabolite (natural product) and principal alkaloid of the ergot fungus, Claviceps purpurea, and related fungi in the family Clavicipitaceae. Ergotamine possesses structural similarity to several neurotransmitters, and has biological activity as a vasoconstrictor. It is used medicinally for treatment of acute migraine attacks (sometimes in combination with caffeine), and to induce childbirth and prevent post-partum haemorrhage. (W737)
Synonyms
  1. 5'-Benzyl-12'-hydroxy-2'-methyl-3',6',18-trioxoergotaman
  2. Cornutamine
  3. Ergotamine
  4. Ergonsvine
  5. Ergostat
  6. Ergotamin
  7. Ergotamina
  8. Ergotamina [spanish]
  9. Ergotamine bitartrate
  10. Ergotaminum
  11. Ergotaminum [latin]
  12. Ergoton-a [as succinate]
  13. Gynergen
  14. Rigetamin
  15. Temigran
Chemical IUPAC Name N-{7-benzyl-2-hydroxy-4-methyl-5,8-dioxo-3-oxa-6,9-diazatricyclo[7.3.0.0^{2,6}]dodecan-4-yl}-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(15),2,9,12(16),13-pentaene-4-carboxamide
Chemical Formula C33H35N5O5
Chemical Structure Structure
CAS Registry Number 113-15-5
InChI Identifier InChI=1S/C33H35N5O5/c1-32(35-29(39)21-15-23-22-10-6-11-24-28(22)20(17-34-24)16-25(23)36(2)18-21)31(41)38-26(14-19-8-4-3-5-9-19)30(40)37-13-7-12-27(37)33(38,42)43-32/h3-6,8-11,15,17,21,25-27,34,42H,7,12-14,16,18H2,1-2H3,(H,35,39)
InChI Key InChIKey=XCGSFFUVFURLIX-UHFFFAOYSA-N
PubChem Compound ID 8223 Link Image
KEGG ID C07544 Link Image
UniProt ID Not Available
OMIM ID Not Available
ChEBI ID 4826 Link Image
BioCyc ID Not Available
SuperToxic ID Not Available
CTD ID D004878 Link Image
Stitch ID Ergotamine Link Image
DrugBank ID DB00696 Link Image
PDB ID Not Available
ACToR ID Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Ergotamine Link Image
Monoisotopic Mass 581.263819
MOL File Show
PDB File Show
SDF File Show
SMILES CN1CC(C=C2C1CC1=CNC3=C1C2=CC=C3)C(=O)NC1(C)OC2(O)C3CCCN3C(=O)C(CC3=CC=CC=C3)N2C1=O
Appearance Ergomar® Sublingual Tablets are round, green tablets each containing 2 mg of ergotamine tartrate.
Melting Point 213.5 oC
Solubility Slight
Predicted LogP 2.5977
Route of Exposure Oral, dermal, inhalation, and parenteral (contaminated drugs). (W967)
Mechanism of Action Ergoline alkaloids tend to act as a group, producing complex and variable effects of partial agonism or antagonism at adrenergic, dopaminergic, and serotonergic receptors. Variables relating to these effects are influenced by the agent, dosage, species, tissue, physiological, and endocrinological state, and experimental conditions. In particular, ergoline alkaloids have been shown to have the significant affinity towards the 5-HT1 and 5-HT2 serotonin receptors, D1 and D2 dopamine receptors, and alpha-adrenergic receptors. This can result in a number of different effects, including vasoconstriction, convulsions, and hallucinations. Ergometrine is also known to have a non-receptor specific oxytocic activity. Ergotamine acts on migraine by one of two proposed mechanisms: 1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leading to vasoconstriction, which correlates with the relief of migraine headache, and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system, resulting in the inhibition of pro-inflammatory neuropeptide release. (W726, W727, W728)
Metabolism Ergotamine is metabolized by the liver by largely undefined pathways, and 90% of the metabolites are excreted in the bile. (U191)
Toxicity Values LD50: 62 mg/kg (Intravenous, Rat) (S448)
Lethal Dose Not Available
Carcinogenicity (IARC Classification) Not Available
Uses/Sources Ergotamine is a secondary metabolite (natural product) and principal alkaloid of the ergot fungus, Claviceps purpurea, and related fungi in the family Clavicipitaceae. It is used medicinally for treatment of acute migraine attacks (sometimes in combination with caffeine), and to induce childbirth and prevent post-partum haemorrhage. (W737)
Minimum Risk Level Not Available
Health Effects Vasoconstrictive complications of a serious nature may occur at times. These include ischemia, cyanosis, absence of pulse, cold extremities, gangrene, precordial distress and pain, EKG changes and muscle pains. Although these effects occur most commonly with long-term therapy at relatively high doses, they have also been reported with short-term or normal doses. Other cardiovascular adverse effects include transient tachycardia or bradycardia and hypertension. Ingestion of ergoline alkaloids is also known to cause the disease ergotism. Ergotism occurs in two forms, gangrenous and convulsive, likely depending on the different kinds and amounts of ergoline alkaloids present. (U191, U190, W723)
Symptoms Signs of ergotamine overexposure include irritation, nausea, vomiting, headache, diarrhea, thirst, coldness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion. Convulsive ergotism can cause painful seizures and spasms, diarrhea, paresthesias, itching, headaches, nausea and vomiting. Usually the gastrointestinal effects precede the central nervous system effects. As well as seizures there can be hallucinations and mental effects including mania or psychosis. Gangrenous ergotism causes dry gangrene as a result of vasoconstriction induced in the more poorly vascularized distal structures, such as the fingers and toes. Symptoms include desquamation, weak periphery pulse, loss of peripheral sensation, edema and ultimately the death and loss of affected tissues. (U191, V687, W724)
Treatment Treatment consists of removal of the offending drug. Maintenance of adequate pulmonary ventilation, correction of hypotension, and control of convulsions and blood pressure are important considerations. Treatment of peripheral vasospasm should consist of warmth, but not heat, and protection of the ischemic limbs. Vasodilators may be beneficial but caution must be exercised to avoid aggravating an already existent hypotension. (V687)
General References
  • W967 - Peraica M, Domijan AM. Contamination of food with mycotoxins and human health. Arh Hig Rada Toksikol. 2001 Mar;52(1):23-35. [PubMed Link Image]
  • W727 - Schiff PL. Ergot and its alkaloids. Am J Pharm Educ. 2006 Oct 15;70(5):98. [PubMed Link Image]
  • V687 - RxList: The Internet Drug Index (2009).
  • U190 - Drugs.com
  • U191 - Tfelt-Hansen P, Saxena PR, Dahlof C, Pascual J, Lainez M, Henry P, Diener H, Schoenen J, Ferrari MD, Goadsby PJ: Ergotamine in the acute treatment of migraine: a review and European consensus. Brain. 2000 Jan;123 ( Pt 1):9-18. [PubMed Link Image]
  • U192 - Schardl CL, Panaccione DG, Tudzynski P: Ergot alkaloids--biology and molecular biology. Alkaloids Chem Biol. 2006;63:45-86. [PubMed Link Image]
  • W737 - Wikipedia. Ergotamine. Last Updated 20 April 2010. []
  • W724 - Wikipedia. Ergotism. Last Updated 6 April 2010. []
  • W728 - Kvernmo T, Härtter S, Burger E. A review of the receptor-binding and pharmacokinetic properties of dopamine agonists. Clin Ther. 2006 Aug;28(8):1065-78. [PubMed Link Image]
  • W723 - Toxicology of mycotoxins. Some major mycotoxins and their mycotoxicoses--an overview. Int J Food Microbiol. 2007 Oct 20;119(1-2):3-10. Epub 2007 Jul 31. [PubMed Link Image]
  • W726 - Mantegani S, Brambilla E, Varasi M. Ergoline derivatives: receptor affinity and selectivity. Farmaco. 1999 May 30;54(5):288-96. [PubMed Link Image]
Targets
  1. Alpha-1A adrenergic receptor
  2. 5-hydroxytryptamine receptor 1D
  3. 5-hydroxytryptamine receptor 1B
  4. 5-hydroxytryptamine receptor 2A
  5. Alpha-2A adrenergic receptor
  6. D(2) dopamine receptor
  7. Alpha-2B adrenergic receptor
  8. 5-hydroxytryptamine receptor 2B
  9. 5-hydroxytryptamine receptor 2C
  10. Alpha-1B adrenergic receptor
  11. Alpha-1D adrenergic receptor
  12. Alpha-2C adrenergic receptor
Target 1 [top]
Target 1 ID 1142
Target 1 Name Alpha-1A adrenergic receptor
Target 1 Mechanism of Action Ergotamine acts as an agonist at alpha-adrenergic receptors, causing vasoconstriction. (S911, S912, U198)
Target 1 Description This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins
Target 1 Synonyms
  1. Alpha 1A-adrenoreceptor; Alpha 1A-adrenoceptor; Alpha-1C adrenergic receptor; Alpha-adrenergic receptor 1c
Target 1 Gene Name ADRA1A
Target 1 Protein Sequence >Alpha-1A adrenergic receptor 
MVFLSGNASDSSNCTQPPAPVNISKAILLGVILGGLILFGVLGNILVILSVACHRHLHSV
THYYIVNLAVADLLLTSTVLPFSAIFEVLGYWAFGRVFCNIWAAVDVLCCTASIMGLCII
SIDRYIGVSYPLRYPTIVTQRRGLMALLCVWALSLVISIGPLFGWRQPAPEDETICQINE
EPGYVLFSALGSFYLPLAIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKN
APAGGSGMASAKTKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPD
FKPSETVFKIVFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLCRKQSSKHALGYTL
HPPSQAVEGQHKDMVRIPVGSRETFYRISKTDGVCEWKFFSSMPRGSARITVSKDQSSCT
TARVRSKSFLQVCCCVGPSTPSLDKNHQVPTIKVHTISLSENGEEV
Target 1 Number of Residues 466
Target 1 Molecular Weight 51486.0
Target 1 Theoretical pI 9.23
Target 1 GO Classification
Function
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-adrenergic receptor activity
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 alpha1-adrenergic receptor activity
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 28-51
  • 65-88
  • 100-122
  • 144-167
  • 182-205
  • 274-297
  • 306-329
Target 1 Essentiality Non Essential
Target 1 Domain Function PF00001:7tm_1
Target 1 GenBank ID Protein Not Available
Target 1 UniProtKB ID P35348 Link Image
Target 1 Cellular Location Cell membrane
Target 1 Gene Sequence >1401 bp 
ATGGTGTTTCTCTCGGGAAATGCTTCCGACAGCTCCAACTGCACCCAACCGCCGGCACCG
GTGAACATTTCCAAGGCCATTCTGCTCGGGGTGATCTTGGGGGGCCTCATTCTTTTCGGG
GTGCTGGGTAACATCCTAGTGATCCTCTCCGTAGCCTGTCACCGACACCTGCACTCAGTC
ACGCACTACTACATCGTCAACCTGGCGGTGGCCGACCTCCTGCTCACCTCCACGGTGCTG
CCCTTCTCCGCCATCTTCGAGGTCCTAGGCTACTGGGCCTTCGGCAGGGTCTTCTGCAAC
ATCTGGGCGGCAGTGGATGTGCTGTGCTGCACCGCGTCCATCATGGGCCTCTGCATCATC
TCCATCGACCGCTACATCGGCGTGAGCTACCCGCTGCGCTACCCAACCATCGTCACCCAG
AGGAGGGGTCTCATGGCTCTGCTCTGCGTCTGGGCACTCTCCCTGGTCATATCCATTGGA
CCCCTGTTCGGCTGGAGGCAGCCGGCCCCCGAGGACGAGACCATCTGCCAGATCAACGAG
GAGCCGGGCTACGTGCTCTTCTCAGCGCTGGGCTCCTTCTACCTGCCTCTGGCCATCATC
CTGGTCATGTACTGCCGCGTCTACGTGGTGGCCAAGAGGGAGAGCCGGGGCCTCAAGTCT
GGCCTCAAGACCGACAAGTCGGACTCGGAGCAAGTGACGCTCCGCATCCATCGGAAAAAC
GCCCCGGCAGGAGGCAGCGGGATGGCCAGCGCCAAGACCAAGACGCACTTCTCAGTGAGG
CTCCTCAAGTTCTCCCGGGAGAAGAAAGCGGCCAAAACGCTGGGCATCGTGGTCGGCTGC
TTCGTCCTCTGCTGGCTGCCTTTTTTCTTAGTCATGCCCATTGGGTCTTTCTTCCCTGAT
TTCAAGCCCTCTGAAACAGTTTTTAAAATAGTATTTTGGCTCGGATATCTAAACAGCTGC
ATCAACCCCATCATATACCCATGCTCCAGCCAAGAGTTCAAAAAGGCCTTTCAGAATGTC
TTGAGAATCCAGTGTCTCCGCAGAAAGCAGTCTTCCAAACATGCCCTGGGCTACACCCTG
CACCCGCCCAGCCAGGCCGTGGAAGGGCAACACAAGGACATGGTGCGCATCCCCGTGGGA
TCAAGAGAGACCTTCTACAGGATCTCCAAGACGGATGGCGTTTGTGAATGGAAATTTTTC
TCTTCCATGCCCCGTGGATCTGCCAGGATTACAGTGTCCAAAGACCAATCCTCCTGTACC
ACAGCCCGGGTGAGAAGTAAAAGCTTTTTGGAGGTCTGCTGCTGTGTAGGGCCCTCAACC
CCCAGCCTTGACAAGAACCATCAAGTTCCAACCATTAAGGTCCACACCATCTCCCTCAGT
GAGAACGGGGAGGAAGTCTAG
Target 1 GenBank Gene ID Not Available
Target 1 GeneCard ID ADRA1A Link Image
Target 1 GenAtlas ID ADRA1A Link Image
Target 1 HGNC ID HGNC:277 Link Image
Target 1 Chromosome Location Not Available
Target 1 Locus 8p21-p11.2
Target 1 SNPs SNPJam Report Link Image
Target 1 Toxin References
  • S912 - 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 Link Image]
  • U198 - Valdivia LF, Centurion D, Arulmani U, Saxena PR, Villalon CM: 5-HT1B receptors, alpha2A/2C- and, to a lesser extent, alpha1-adrenoceptors mediate the external carotid vasoconstriction to ergotamine in vagosympathectomised dogs. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):46-53. Epub 2004 Jun 29. [PubMed Link Image]
  • W738 - Görnemann T, Jähnichen S, Schurad B, Latté KP, Horowski R, Tack J, Flieger M, Pertz HH. Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jan;376(5):321-30. Epub 2007 Dec 8. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 1 General References 8396931; 8024574; 8183249; 8564208; 7815325; 7737411; 9490024; 10493934
Target 2 [top]
Target 2 ID 1163
Target 2 Name 5-hydroxytryptamine receptor 1D
Target 2 Mechanism of Action Ergotamine acts as an agonist at 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leading to vasoconstriction. It also activates 5-HT1D receptors on sensory nerve endings of the trigeminal system, resulting in the inhibition of pro-inflammatory neuropeptide release. (T550, U194, T551, U195, U196)
Target 2 Description 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 Synonyms
  1. 5-HT-1D; 5-HT-1D-alpha; Serotonin receptor 1D
Target 2 Gene Name HTR1D
Target 2 Protein Sequence >5-hydroxytryptamine receptor 1D 
MSPLNQSAEGLPQEASNRSLNATETSEAWDPRTLQALKISLAVVLSVITLATVLSNAFVL
TTILLTRKLHTPANYLIGSLATTDLLVSILVMPISIAYTITHTWNFGQILCDIWLSSDIT
CCTASILHLCVIALDRYWAITDALEYSKRRTAGHAATMIAIVWAISICISIPPLFWRQAK
AQEEMSDCLVNTSQISYTIYSTCGAFYIPSVLLIILYGRIYRAARNRILNPPSLYGKRFT
TAHLITGSAGSSLCSLNSSLHEGHSHSAGSPLFFNHVKIKLADSALERKRISAARERKAT
KILGIILGAFIICWLPFFVVSLVLPICRDSCWIHPALFDFFTWLGYLNSLINPIIYTVFN
EEFRQAFQKIVPFRKAS
Target 2 Number of Residues 377
Target 2 Molecular Weight 41906.4
Target 2 Theoretical pI 8.85
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 serotonin receptor activity
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 39-62
  • 76-98
  • 109-134
  • 155-176
  • 195-218
  • 303-326
  • 336-360
Target 2 Essentiality Non Essential
Target 2 Domain Function PF00001:7tm_1
Target 2 GenBank ID Protein Not Available
Target 2 UniProtKB ID P28221 Link Image
Target 2 Cellular Location Cell membrane
Target 2 Gene Sequence >1134 bp 
ATGTCCCCACTGAACCAGTCAGCAGAAGGCCTTCCCCAGGAGGCCTCCAACAGATCCCTG
AATGCCACAGAAACCTCAGAGGCTTGGGATCCCAGGACCCTCCAGGCGCTCAAGATCTCC
CTTGCCGTGGTCCTTTCCGTCATCACACTGGCCACAGTCCTCTCCAATGCCTTTGTACTC
ACCACCATCTTACTCACCAGGAAGCTCCACACCCCTGCCAACTACCTGATTGGCTCCCTG
GCCACCACCGACCTCTTGGTTTCCATCTTGGTAATGCCCATCAGCATCGCCTATACCATC
ACCCACACCTGGAACTTTGGCCAAATCTTGTGTGACATCTGGCTGTCCTCTGACATCACG
TGCTGCACAGCCTCCATCCTGCATCTCTGTGTCATTGCTCTGGACAGGTACTGGGCAATC
ACAGATGCCCTGGAATACAGTAAACGCAGGACGGCTGGCCACGCGGCCACCATGATCGCC
ATTGTCTGGGCCATCTCCATCTGCATCTCCATCCCCCCGCTCTTCTGGCGGCAGGCCAAG
GCCCAGGAGGAGATGTCGGACTGTCTGGTGAACACCTCTCAGATCTCCTACACCATCTAC
TCCACCTGTGGGGCCTTCTACATTCCCTCGGTGTTGCTCATCATCCTATATGGCCGGATC
TACCGGGCTGCCCGGAACCGCATCCTGAATCCACCCTCACTCTATGGGAAGCGCTTCACC
ACGGCCCACCTCATCACAGGCTCTGCCGGGTCCTCGCTCTGCTCGCTCAACTCCAGCCTC
CATGAGGGGCACTCGCACTCGGCTGGCTCCCCTCTCTTTTTCAACCACGTGAAAATCAAG
CTTGCTGACAGTGCCCTGGAACGCAAGAGGATTTCTGCTGCTCGAGAAAGGAAAGCCACT
AAAATCCTGGGCATCATTCTGGGGGCCTTTATCATCTGCTGGCTGCCCTTCTTCGTGGTG
TCTCTGGTCCTCCCCATCTGCCGGGACTCCTGCTGGATCCACCCGGCGCTCTTTGACTTC
TTCACCTGGCTAGGCTATTTAAACTCCCTCATCAATCCAATAATCTACACTGTGTTTAAT
GAAGAGTTTCGGCAAGCTTTTCAGAAAATTGTCCCTTTCCGGAAGGCCTCCTAG
Target 2 GenBank Gene ID Not Available
Target 2 GeneCard ID HTR1D Link Image
Target 2 GenAtlas ID HTR1D Link Image
Target 2 HGNC ID HGNC:5289 Link Image
Target 2 Chromosome Location Not Available
Target 2 Locus 1p36.3-p34.3
Target 2 SNPs SNPJam Report Link Image
Target 2 Toxin References
  • U195 - Sanchez-Lopez A, Centurion D, Vazquez E, Arulmani U, Saxena PR, Villalon CM: Pharmacological profile of the 5-HT-induced inhibition of cardioaccelerator sympathetic outflow in pithed rats: correlation with 5-HT1 and putative 5-ht5A/5B receptors. Br J Pharmacol. 2003 Oct;140(4):725-35. Epub 2003 Sep 22. [PubMed Link Image]
  • U196 - Deliganis AV, Peroutka SJ: 5-Hydroxtryptamine1D receptor agonism predicts antimigraine efficacy. Headache. 1991 Apr;31(4):228-31. [PubMed Link Image]
  • T551 - Hoyer D, Lery H, Waeber C, Bruinvels AT, Nozulak J, Palacios JM: "5-HT1R" or 5-HT1D sites? Evidence for 5-HT1D binding sites in rabbit brain. Naunyn Schmiedebergs Arch Pharmacol. 1992 Sep;346(3):249-54. [PubMed Link Image]
  • T550 - Silberstein SD, McCrory DC: Ergotamine and dihydroergotamine: history, pharmacology, and efficacy. Headache. 2003 Feb;43(2):144-66. [PubMed Link Image]
  • U194 - 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 General References 1652050; 1565658; 16710414; 15489334; 10391209
Target 3 [top]
Target 3 ID 1167
Target 3 Name 5-hydroxytryptamine receptor 1B
Target 3 Mechanism of Action Ergotamine acts as an agonist at 5-HT1B receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leading to vasoconstriction. It also activates 5-HT1B receptors on sensory nerve endings of the trigeminal system, resulting in the inhibition of pro-inflammatory neuropeptide release. (U197, T552, U150, U198)
Target 3 Description 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 Synonyms
  1. 5-HT-1D-beta; 5-HT-1B; 5-HT1B; Serotonin receptor 1B; Serotonin 1D beta receptor; S12
Target 3 Gene Name HTR1B
Target 3 Protein Sequence >5-hydroxytryptamine receptor 1B 
MEEPGAQCAPPPPAGSETWVPQANLSSAPSQNCSAKDYIYQDSISLPWKVLLVMLLALIT
LATTLSNAFVIATVYRTRKLHTPANYLIASLAVTDLLVSILVMPISTMYTVTGRWTLGQV
VCDFWLSSDITCCTASILHLCVIALDRYWAITDAVEYSAKRTPKRAAVMIALVWVFSISI
SLPPFFWRQAKAEEEVSECVVNTDHILYTVYSTVGAFYFPTLLLIALYGRIYVEARSRIL
KQTPNRTGKRLTRAQLITDSPGSTSSVTSINSRVPDVPSESGSPVYVNQVKVRVSDALLE
KKKLMAARERKATKTLGIILGAFIVCWLPFFIISLVMPICKDACWFHLAIFDFFTWLGYL
NSLINPIIYTMSNEDFKQAFHKLIRFKCTS
Target 3 Number of Residues 390
Target 3 Molecular Weight 43567.5
Target 3 Theoretical pI 8.82
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 protein binding
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 50-73
  • 87-109
  • 120-145
  • 166-187
  • 206-229
  • 316-340
  • 348-373
Target 3 Essentiality Non Essential
Target 3 Domain Function PF00001:7tm_1
Target 3 GenBank ID Protein Not Available
Target 3 UniProtKB ID P28222 Link Image
Target 3 Cellular Location Cell membrane
Target 3 Gene Sequence >1173 bp 
ATGGAGGAACCGGGTGCTCAGTGCGCTCCACCGCCGCCCGCGGGCTCCGAGACCTGGGTT
CCTCAAGCCAACTTATCCTCTGCTCCCTCCCAAAACTGCAGCGCCAAGGACTACATTTAC
CAGGACTCCATCTCCCTACCCTGGAAAGTACTGCTGGTTATGCTATTGGCGCTCATCACC
TTGGCCACCACGCTCTCCAATGCCTTTGTGATTGCCACAGTGTACCGGACCCGGAAACTG
CACACCCCGGCTAACTACCTGATCGCCTCTCTGGCAGTCACCGACCTGCTTGTGTCCATC
CTGGTGATGCCCATCAGCACCATGTACACTGTCACCGGCCGCTGGACACTGGGCCAGGTG
GTCTGTGACTTCTGGCTGTCGTCGGACATCACTTGTTGCACTGCCTCCATCCTGCACCTC
TGTGTCATCGCCCTGGACCGCTACTGGGCCATCACGGACGCCGTGGAGTACTCAGCTAAA
AGGACTCCCAAGAGGGCGGCGGTCATGATCGCGCTGGTGTGGGTCTTCTCCATCTCTATC
TCGCTGCCGCCCTTCTTCTGGCGTCAGGCTAAGGCCGAAGAGGAGGTGTCGGAATGCGTG
GTGAACACCGACCACATCCTCTACACGGTCTACTCCACGGTGGGTGCTTTCTACTTCCCC
ACCCTGCTCCTCATCGCCCTCTATGGCCGCATCTACGTAGAAGCCCGCTCCCGGATTTTG
AAACAGACGCCCAACAGGACCGGCAAGCGCTTGACCCGAGCCCAGCTGATAACCGACTCC
CCCGGGTCCACGTCCTCGGTCACCTCTATTAACTCGCGGGTTCCCGACGTGCCCAGCGAA
TCCGGATCTCCTGTGTATGTGAACCAAGTCAAAGTGCGAGTCTCCGACGCCCTGCTGGAA
AAGAAGAAACTCATGGCCGCTAGGGAGCGCAAAGCCACCAAGACCCTAGGGATCATTTTG
GGAGCCTTTATTGTGTGTTGGCTACCCTTCTTCATCATCTCCCTAGTGATGCCTATCTGC
AAAGATGCCTGCTGGTTCCACCTAGCCATCTTTGACTTCTTCACATGGCTGGGCTATCTC
AACTCCCTCATCAACCCCATAATCTATACCATGTCCAATGAGGACTTTAAACAAGCATTC
CATAAACTGATACGTTTTAAGTGCACAAGTTGA
Target 3 GenBank Gene ID Not Available
Target 3 GeneCard ID HTR1B Link Image
Target 3 GenAtlas ID HTR1B Link Image
Target 3 HGNC ID HGNC:5287 Link Image
Target 3 Chromosome Location Not Available
Target 3 Locus 6q13
Target 3 SNPs SNPJam Report Link Image
Target 3 Toxin References
  • T552 - Willems EW, Trion M, De Vries P, Heiligers JP, Villalon CM, Saxena PR: Pharmacological evidence that alpha1-and alpha2-adrenoceptors mediate vasoconstriction of carotid arteriovenous anastomoses in anaesthetized pigs. Br J Pharmacol. 1999 Jul;127(5):1263-71. [PubMed Link Image]
  • U198 - Valdivia LF, Centurion D, Arulmani U, Saxena PR, Villalon CM: 5-HT1B receptors, alpha2A/2C- and, to a lesser extent, alpha1-adrenoceptors mediate the external carotid vasoconstriction to ergotamine in vagosympathectomised dogs. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):46-53. Epub 2004 Jun 29. [PubMed Link Image]
  • U150 - 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]
  • U197 - Villalon CM, De Vries P, Rabelo G, Centurion D, Sanchez-Lopez A, Saxena P: Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors. Br J Pharmacol. 1999 Feb;126(3):585-94. [PubMed Link Image]
Target 3 General References 1315531; 1610347; 1348246; 1559993; 1565658; 1351684; 1328844; 15014171; 14574404
Target 4 [top]
Target 4 ID 788
Target 4 Name 5-hydroxytryptamine receptor 2A
Target 4 Mechanism of Action Ergotamine acts as an agonist at 5-HT2 receptors, causing vasoconstriction. (U199, U200, S918)
Target 4 Description 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. This receptor is involved in tracheal smooth muscle contraction, bronchoconstriction, and control of aldosterone production
Target 4 Synonyms
  1. 5-HT-2A; 5-HT-2; Serotonin receptor 2A
Target 4 Gene Name HTR2A
Target 4 Protein Sequence >5-hydroxytryptamine receptor 2A 
MDILCEENTSLSSTTNSLMQLNDDTRLYSNDFNSGEANTSDAFNWTVDSENRTNLSCEGC
LSPSCLSLLHLQEKNWSALLTAVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIAD
MLLGFLVMPVSMLTILYGYRWPLPSKLCAVWIYLDVLFSTASIMHLCAISLDRYVAIQNP
IHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSF
VSFFIPLTIMVITYFLTIKSLQKEATLCVSDLGTRAKLASFSFLPQSSLSSEKLFQRSIH
REPGSYTGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNEDVIGA
LLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENKKPLQLILVNTIPALAYK
SSQLQMGQKKNSKQDAKTTDNDCSMVALGKQHSEEASKDNSDGVNEKVSCV
Target 4 Number of Residues 471
Target 4 Molecular Weight 52602.6
Target 4 Theoretical pI 7.72
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 serotonin binding
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • 76-99
  • 111-132
  • 148-171
  • 192-215
  • 234-254
  • 325-346
  • 363-384
Target 4 Essentiality Non Essential
Target 4 Domain Function PF00001:7tm_1
Target 4 GenBank ID Protein Not Available
Target 4 UniProtKB ID P28223 Link Image
Target 4 Cellular Location Cell membrane
Target 4 Gene Sequence >1416 bp 
ATGGATATTCTTTGTGAAGAAAATACTTCTTTGAGCTCAACTACGAACTCCCTAATGCAA
TTAAATGATGACACCAGGCTCTACAGTAATGACTTTAACTCTGGAGAAGCTAACACTTCT
GATGCATTTAACTGGACAGTCGACTCTGAAAATCGAACCAACCTTTCCTGTGAAGGGTGC
CTCTCACCGTCGTGTCTCTCCTTACTTCATCTCCAGGAAAAAAACTGGTCTGCTTTACTG
ACAGCCGTAGTGATTATTCTAACTATTGCTGGAAACATACTCGTCATCATGGCAGTGTCC
CTAGAGAAAAAGCTGCAGAATGCCACCAACTATTTCCTGATGTCACTTGCCATAGCTGAT
ATGCTGCTGGGTTTCCTTGTCATGCCCGTGTCCATGTTAACCATCCTGTATGGGTACCGG
TGGCCTCTGCCGAGCAAGCTTTGTGCAGTCTGGATTTACCTGGACGTGCTCTTCTCCACG
GCCTCCATCATGCACCTCTGCGCCATCTCGCTGGACCGCTACGTCGCCATCCAGAATCCC
ATCCACCACAGCCGCTTCAACTCCAGAACTAAGGCATTTCTGAAAATCATTGCTGTTTGG
ACCATATCAGTAGGTATATCCATGCCAATACCAGTCTTTGGGCTACAGGACGATTCGAAG
GTCTTTAAGGAGGGGAGTTGCTTACTCGCCGATGATAACTTTGTCCTGATCGGCTCTTTT
GTGTCATTTTTCATTCCCTTAACCATCATGGTGATCACCTACTTTCTAACTATCAAGTCA
CTCCAGAAAGAAGCTACTTTGTGTGTAAGTGATCTTGGCACACGGGCCAAATTAGCTTCT
TTCAGCTTCCTCCCTCAGAGTTCTTTGTCTTCAGAAAAGCTCTTCCAGCGGTCGATCCAT
AGGGAGCCAGGGTCCTACACAGGCAGGAGGACTATGCAGTCCATCAGCAATGAGCAAAAG
GCATGCAAGGTGCTGGGCATCGTCTTCTTCCTGTTTGTGGTGATGTGGTGCCCTTTCTTC
ATCACAAACATCATGGCCGTCATCTGCAAAGAGTCCTGCAATGAGGATGTCATTGGGGCC
CTGCTCAATGTGTTTGTTTGGATCGGTTATCTCTCTTCAGCAGTCAACCCACTAGTCTAC
ACACTGTTCAACAAGACCTATAGGTCAGCCTTTTCACGGTATATTCAGTGTCAGTACAAG
GAAAACAAAAAACCATTGCAGTTAATTTTAGTGAACACAATACCGGCTTTGGCCTACAAG
TCTAGCCAACTTCAAATGGGACAAAAAAAGAATTCAAAGCAAGATGCCAAGACAACAGAT
AATGACTGCTCAATGGTTGCTCTAGGAAAGCAGCATTCTGAAGAGGCTTCTAAAGACAAT
AGCGACGGAGTGAATGAAAAGGTGAGCTGTGTGTGA
Target 4 GenBank Gene ID Not Available
Target 4 GeneCard ID HTR2A Link Image
Target 4 GenAtlas ID HTR2A Link Image
Target 4 HGNC ID HGNC:5293 Link Image
Target 4 Chromosome Location Chromosome:13
Target 4 Locus 13q14-q21
Target 4 SNPs SNPJam Report Link Image
Target 4 Toxin References
  • S918 - Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  • U200 - Panconesi A, Anselmi B, Curradi C, Perfetto F, Piluso A, Franchi G: Comparison between venoconstrictor effects of sumatriptan and ergotamine in migraine patients. Headache. 1994 Apr;34(4):194-7. [PubMed Link Image]
  • U199 - Bom AH, Heiligers JP, Saxena PR, Verdouw PD: Reduction of cephalic arteriovenous shunting by ergotamine is not mediated by 5-HT1-like or 5-HT2 receptors. Br J Pharmacol. 1989 Jun;97(2):383-90. [PubMed Link Image]
Target 4 General References 1722404; 1323014; 8035173; 15057823; 15489334; 1330647; 11150294; 14988405
Target 5 [top]
Target 5 ID 1143
Target 5 Name Alpha-2A adrenergic receptor
Target 5 Mechanism of Action Ergotamine acts as an agonist at alpha-adrenergic receptors, causing vasoconstriction. (S911, S912, U198)
Target 5 Description Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol
Target 5 Synonyms
  1. Alpha-2A adrenoreceptor; Alpha-2A adrenoceptor; Alpha-2AAR; Alpha-2 adrenergic receptor subtype C10
Target 5 Gene Name ADRA2A
Target 5 Protein Sequence >Alpha-2A adrenergic receptor 
MGSLQPDAGNASWNGTEAPGGGARATPYSLQVTLTLVCLAGLLMLLTVFGNVLVIIAVFT
SRALKAPQNLFLVSLASADILVATLVIPFSLANEVMGYWYFGKAWCEIYLALDVLFCTSS
IVHLCAISLDRYWSITQAIEYNLKRTPRRIKAIIITVWVISAVISFPPLISIEKKGGGGG
PQPAEPRCEINDQKWYVISSCIGSFFAPCLIMILVYVRIYQIAKRRTRVPPSRRGPDAVA
APPGGTERRPNGLGPERSAGPGGAEAEPLPTQLNGAPGEPAPAGPRDTDALDLEESSSSD
HAERPPGPRRPERGPRGKGKARASQVKPGDSLPRRGPGATGIGTPAAGPGEERVGAAKAS
RWRGRQNREKRFTFVLAVVIGVFVVCWFPFFFTYTLTAVGCSVPRTLFKFFFWFGYCNSS
LNPVIYTIFNHDFRRAFKKILCRGDRKRIV
Target 5 Number of Residues 450
Target 5 Molecular Weight 48956.3
Target 5 Theoretical pI 10.20
Target 5 GO Classification
Function
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha2-adrenergic receptor activity
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 5 General Function Involved in alpha2-adrenergic receptor activity
Target 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Signals
  • None
Target 5 Transmembrane Regions
  • 34-59
  • 71-96
  • 107-129
  • 152-172
  • 195-217
  • 375-395
  • 410-429
Target 5 Essentiality Non Essential
Target 5 Domain Function PF00001:7tm_1
Target 5 GenBank ID Protein Not Available
Target 5 UniProtKB ID P08913 Link Image
Target 5 Cellular Location Cell membrane
Target 5 Gene Sequence >1353 bp 
ATGGGCTCCCTGCAGCCGGACGCGGGCAACGCGAGCTGGAACGGGACCGAGGCGCCGGGG
GGCGGCGCCCGGGCCACCCCTTACTCCCTGCAGGTGACGCTGACGCTGGTGTGCCTGGCC
GGCCTGCTCATGCTGCTCACCGTGTTCGGCAACGTGCTCGTCATCATCGCCGTGTTCACG
AGCCGCGCGCTCAAGGCGCCCCAAAACCTCTTCCTGGTGTCTCTGGCCTCGGCCGACATC
CTGGTGGCCACGCTCGTCATCCCTTTCTCGCTGGCCAACGAGGTCATGGGCTACTGGTAC
TTCGGCAAGGCTTGGTGCGAGATCTACCTGGCGCTCGACGTGCTCTTCTGCACGTCGTCC
ATCGTGCACCTGTGCGCCATCAGCCTGGACCGCTACTGGTCCATCACACAGGCCATCGAG
TACAACCTGAAGCGCACGCCGCGCCGCATCAAGGCCATCATCATCACCGTGTGGGTCATC
TCGGCCGTCATCTCCTTCCCGCCGCTCATCTCCATCGAGAAGAAGGGCGGCGGCGGCGGC
CCGCAGCCGGCCGAGCCGCGCTGCGAGATCAACGACCAGAAGTGGTACGTCATCTCGTCG
TGCATCGGCTCCTTCTTCGCTCCCTGCCTCATCATGATCCTGGTCTACGTGCGCATCTAC
CAGATCGCCAAGCGTCGCACCCGCGTGCCACCCAGCCGCCGGGGTCCGGACGCCGTCGCC
GCGCCGCCGGGGGGCACCGAGCGCAGGCCCAACGGTCTGGGCCCCGAGCGCAGCGCGGGC
CCGGGGGGCGCAGAGGCCGAACCGCTGCCCACCCAGCTCAACGGCGCCCCTGGCGAGCCC
GCGCCGGCCGGGCCGCGCGACACCGACGCGCTGGACCTGGAGGAGAGCTCGTCTTCCGAC
CACGCCGAGCGGCCTCCAGGGCCCCGCAGACCCGAGCGCGGTCCCCGGGGCAAAGGCAAG
GCCCGAGCGAGCCAGGTGAAGCCGGGCGACAGCCTGCCGCGGCGCGGGCCGGGGGCGACG
GGGATCGGGACGCCGGCTGCAGGGCCGGGGGAGGAGCGCGTCGGGGCTGCCAAGGCGTCG
CGCTGGCGCGGGCGGCAGAACCGCGAGAAGCGCTTCACGTTCGTGCTGGCCGTGGTCATC
GGAGTGTTCGTGGTGTGCTGGTTCCCCTTCTTCTTCACCTACACGCTCACGGCCGTCGGG
TGCTCCGTGCCACGCACGCTCTTCAAATTCTTCTTCTGGTTCGGCTACTGCAACAGCTCG
TTGAACCCGGTCATCTACACCATCTTCAACCACGATTTCCGCCGCGCCTTCAAGAAGATC
CTCTGTCGGGGGGACAGGAAGCGGATCGTGTGA
Target 5 GenBank Gene ID Not Available
Target 5 GeneCard ID ADRA2A Link Image
Target 5 GenAtlas ID ADRA2A Link Image
Target 5 HGNC ID HGNC:281 Link Image
Target 5 Chromosome Location Chromosome:10
Target 5 Locus 10q24-q26
Target 5 SNPs SNPJam Report Link Image
Target 5 Toxin References
  • S912 - 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 Link Image]
  • U198 - Valdivia LF, Centurion D, Arulmani U, Saxena PR, Villalon CM: 5-HT1B receptors, alpha2A/2C- and, to a lesser extent, alpha1-adrenoceptors mediate the external carotid vasoconstriction to ergotamine in vagosympathectomised dogs. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):46-53. Epub 2004 Jun 29. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 5 General References 2823383; 2568356; 2170371; 10948191; 16567612
Target 6 [top]
Target 6 ID 1171
Target 6 Name D(2) dopamine receptor
Target 6 Mechanism of Action Ergotamine acts as an agonist at D(2) dopamine receptors. (U191, U193)
Target 6 Description This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
Target 6 Synonyms
  1. Dopamine D2 receptor
Target 6 Gene Name DRD2
Target 6 Protein Sequence >D(2) dopamine receptor 
MDPLNLSWYDDDLERQNWSRPFNGSDGKADRPHYNYYATLLTLLIAVIVFGNVLVCMAVS
REKALQTTTNYLIVSLAVADLLVATLVMPWVVYLEVVGEWKFSRIHCDIFVTLDVMMCTA
SILNLCAISIDRYTAVAMPMLYNTRYSSKRRVTVMISIVWVLSFTISCPLLFGLNNADQN
ECIIANPAFVVYSSIVSFYVPFIVTLLVYIKIYIVLRRRRKRVNTKRSSRAFRAHLRAPL
KGNCTHPEDMKLCTVIMKSNGSFPVNRRRVEAARRAQELEMEMLSSTSPPERTRYSPIPP
SHHQLTLPDPSHHGLHSTPDSPAKPEKNGHAKDHPKIAKIFEIQTMPNGKTRTSLKTMSR
RKLSQQKEKKATQMLAIVLGVFIICWLPFFITHILNIHCDCNIPPVLYSAFTWLGYVNSA
VNPIIYTTFNIEFRKAFLKILHC
Target 6 Number of Residues 443
Target 6 Molecular Weight 50618.9
Target 6 Theoretical pI 9.85
Target 6 GO Classification
Function
amine receptor activity
dopamine receptor activity
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 6 General Function Involved in dopamine D2 receptor activity
Target 6 Pathways Not Available
Target 6 Reactions Not Available
Target 6 Signals
  • None
Target 6 Transmembrane Regions
  • 38-60
  • 72-97
  • 109-130
  • 152-174
  • 187-210
  • 374-397
  • 406-429
Target 6 Essentiality Non Essential
Target 6 Domain Function PF00001:7tm_1
Target 6 GenBank ID Protein Not Available
Target 6 UniProtKB ID P14416 Link Image
Target 6 Cellular Location Cell membrane
Target 6 Gene Sequence >66 bp 
ATGCGGCGGGAGCTGGAAGCCTCAAGCAGCCGGCGCCGTCTCTGCCCCCGGGGCCCTATG
GCTTGA
Target 6 GenBank Gene ID Not Available
Target 6 GeneCard ID DRD2 Link Image
Target 6 GenAtlas ID DRD2 Link Image
Target 6 HGNC ID HGNC:3023 Link Image
Target 6 Chromosome Location Chromosome:11
Target 6 Locus 11q23
Target 6 SNPs SNPJam Report Link Image
Target 6 Toxin References
  • U191 - Tfelt-Hansen P, Saxena PR, Dahlof C, Pascual J, Lainez M, Henry P, Diener H, Schoenen J, Ferrari MD, Goadsby PJ: Ergotamine in the acute treatment of migraine: a review and European consensus. Brain. 2000 Jan;123 ( Pt 1):9-18. [PubMed Link Image]
  • U193 - Verhoeff NP, Visser WH, Ferrari MD, Saxena PR, van Royen EA: Dopamine D2-receptor imaging with 123I-iodobenzamide SPECT in migraine patients abusing ergotamine: does ergotamine cross the blood brain barrier? Cephalalgia. 1993 Oct;13(5):325-9. [PubMed Link Image]
Target 6 General References 2533064; 2531656; 2138729; 2532362; 2137193; 2144985; 1363862; 1835903; 8471125; 10719223
Target 7 [top]
Target 7 ID 1240
Target 7 Name Alpha-2B adrenergic receptor
Target 7 Mechanism of Action Ergotamine acts as an agonist at alpha-adrenergic receptors, causing vasoconstriction. (S911, S912, U198)
Target 7 Description Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol
Target 7 Synonyms
  1. Alpha-2B adrenoreceptor; Alpha-2B adrenoceptor; Alpha-2 adrenergic receptor subtype C2
Target 7 Gene Name ADRA2B
Target 7 Protein Sequence >Alpha-2B adrenergic receptor 
MDHQDPYSVQATAAIAAAITFLILFTIFGNALVILAVLTSRSLRAPQNLFLVSLAAADIL
VATLIIPFSLANELLGYWYFRRTWCEVYLALDVLFCTSSIVHLCAISLDRYWAVSRALEY
NSKRTPRRIKCIILTVWLIAAVISLPPLIYKGDQGPQPRGRPQCKLNQEAWYILASSIGS
FFAPCLIMILVYLRIYLIAKRSNRRGPRAKGGPGQGESKQPRPDHGGALASAKLPALASV
ASAREVNGHSKSTGEKEEGETPEDTGTRALPPSWAALPNSGQGQKEGVCGASPEDEAEEE
EEEEEEEEECEPQAVPVSPASACSPPLQQPQGSRVLATLRGQVLLGRGVGAIGGQWWRRR
AQLTREKRFTFVLAVVIGVFVLCWFPFFFSYSLGAICPKHCKVPHGLFQFFFWIGYCNSS
LNPVIYTIFNQDFRRAFRRILCRPWTQTAW
Target 7 Number of Residues 450
Target 7 Molecular Weight 49953.1
Target 7 Theoretical pI 8.52
Target 7 GO Classification
Function
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha2-adrenergic receptor activity
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 7 General Function Involved in alpha2-adrenergic receptor activity
Target 7 Pathways Not Available
Target 7 Reactions Not Available
Target 7 Signals
  • None
Target 7 Transmembrane Regions
  • 13-38
  • 50-75
  • 86-108
  • 131-153
  • 170-193
  • 373-396
  • 406-429
Target 7 Essentiality Non Essential
Target 7 Domain Function PF00001:7tm_1
Target 7 GenBank ID Protein Not Available
Target 7 UniProtKB ID P18089 Link Image
Target 7 Cellular Location Cell membrane
Target 7 Gene Sequence >1353 bp 
CCCGCCCCGTCATGGACCACCAGGACCCCTACTCCGTGCAGGCCACAGCGGCCATAGCGG
CGGCCATCACCTTCCTCATTCTCTTTACCATCTTCGGCAACGCTCTGGTCATCCTGGCTG
TGTTGACCAGCCGCTCGCTGCGCGCCCCTCAGAACCTGTTCCTGGTGTCGCTGGCCGCCG
CCGACATCCTGGTGGCCACGCTCATCATCCCTTTCTCGCTGGCCAACGAGCTGCTGGGCT
ACTGGTACTTCCGGCGCACGTGGTGCGAGGTGTACCTGGCGCTCGACGTGCTCTTCTGCA
CCTCGTCCATCGTGCACCTGTGCGCCATCAGCCTGGACCGCTACTGGGCCGTGAGCCGCG
CGCTGGAGTACAACTCCAAGCGCACCCCGCGCCGCATCAAGTGCATCATCCTCACTGTGT
GGCTCATCGCCGCCGTCATCTCGCTGCCGCCCCTCATCTACAAGGGCGACCAGGGCCCCC
AGCCGCGCGGGCGCCCCCAGTGCAAGCTCAACCAGGAGGCCTGGTACATCCTGGCCTCCA
GCATCGGATCTTTCTTTGCTCCTTGCCTCATCATGATCCTTGTCTACCTGCGCATCTACC
TGATCGCCAAACGCAGCAACCGCAGAGGTCCCAGGGCCAAGGGGGGGCCTGGGCAGGGTG
AGTCCAAGCAGCCCCGACCCGACCATGGTGGGGCTTTGGCCTCAGCCAAACTGCCAGCCC
TGGCCTCTGTGGCTTCTGCCAGAGAGGTCAACGGACACTCGAAGTCCACTGGGGAGAAGG
AGGAGGGGGAGACCCCTGAAGATACTGGGACCCGGGCCTTGCCACCCAGTTGGGCTGCCC
TTCCCAACTCAGGCCAGGGCCAGAAGGAGGGTGTTTGTGGGGCATCTCCAGAGGATGAAG
CTGAAGAGGAGGAAGAGGAGGAGGAGGAGGAGGAAGAGTGTGAACCCCAGGCAGTGCCAG
TGTCTCCGGCCTCAGCTTGCAGCCCCCCGCTGCAGCAGCCACAGGGCTCCCGGGTGCTGG
CCACCCTACGTGGCCAGGTGCTCCTGGGCAGGGGCGTGGGTGCTATAGGTGGGCAGTGGT
GGCGTCGAAGGGCGCACGTGACCCGGGAGAAGCGCTTCACCTTCGTGCTGGCTGTGGTCA
TTGGCGTTTTTGTGCTCTGCTGGTTCCCCTTCTTCTTCAGCTACAGCCTGGGCGCCATCT
GCCCGAAGCACTGCAAGGTGCCCCATGGCCTCTTCCAGTTCTTCTTCTGGATCGGCTACT
GCAACAGCTCACTGAACCCTGTTATCTACACCATCTTCAACCAGGACTTCCGCCGTGCCT
TCCGGAGGATCCTGTGCCGCCCGTGGACCCAGA
Target 7 GenBank Gene ID Not Available
Target 7 GeneCard ID ADRA2B Link Image
Target 7 GenAtlas ID ADRA2B Link Image
Target 7 HGNC ID HGNC:282 Link Image
Target 7 Chromosome Location Not Available
Target 7 Locus 2p13-q13
Target 7 SNPs SNPJam Report Link Image
Target 7 Toxin References
  • S912 - 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 Link Image]
  • U198 - Valdivia LF, Centurion D, Arulmani U, Saxena PR, Villalon CM: 5-HT1B receptors, alpha2A/2C- and, to a lesser extent, alpha1-adrenoceptors mediate the external carotid vasoconstriction to ergotamine in vagosympathectomised dogs. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):46-53. Epub 2004 Jun 29. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 7 General References 2164221; 2172775; 11056163; 15037199; 15815621; 2173582
Target 8 [top]
Target 8 ID 790
Target 8 Name 5-hydroxytryptamine receptor 2B
Target 8 Mechanism of Action Ergotamine acts as an agonist at 5-HT2 receptors, causing vasoconstriction. (U199, U200, S918)
Target 8 Description 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 8 Synonyms
  1. 5-HT-2B; Serotonin receptor 2B
Target 8 Gene Name HTR2B
Target 8 Protein Sequence >5-hydroxytryptamine receptor 2B 
MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALL
ILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAM
WPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVW
LISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLT
IHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDET
LMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQM
LLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNP
MAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSY
V
Target 8 Number of Residues 481
Target 8 Molecular Weight 54297.4
Target 8 Theoretical pI 9.47
Target 8 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 8 General Function Involved in serotonin binding
Target 8 Pathways Not Available
Target 8 Reactions Not Available
Target 8 Signals
  • None
Target 8 Transmembrane Regions
  • 57-79
  • 92-113
  • 130-151
  • 172-192
  • 217-239
  • 325-345
  • 361-383
Target 8 Essentiality Non Essential
Target 8 Domain Function PF00001:7tm_1
Target 8 GenBank ID Protein Not Available
Target 8 UniProtKB ID P41595 Link Image
Target 8 Cellular Location Cell membrane
Target 8 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 8 GenBank Gene ID Not Available
Target 8 GeneCard ID HTR2B Link Image
Target 8 GenAtlas ID HTR2B Link Image
Target 8 HGNC ID HGNC:5294 Link Image
Target 8 Chromosome Location Not Available
Target 8 Locus Not Available
Target 8 SNPs SNPJam Report Link Image
Target 8 Toxin References
  • S918 - Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  • U200 - Panconesi A, Anselmi B, Curradi C, Perfetto F, Piluso A, Franchi G: Comparison between venoconstrictor effects of sumatriptan and ergotamine in migraine patients. Headache. 1994 Apr;34(4):194-7. [PubMed Link Image]
  • U199 - Bom AH, Heiligers JP, Saxena PR, Verdouw PD: Reduction of cephalic arteriovenous shunting by ergotamine is not mediated by 5-HT1-like or 5-HT2 receptors. Br J Pharmacol. 1989 Jun;97(2):383-90. [PubMed Link Image]
Target 8 General References 8143856; 7926008; 8078486; 10722792; 15815621; 15489334; 11150294
Target 9 [top]
Target 9 ID 789
Target 9 Name 5-hydroxytryptamine receptor 2C
Target 9 Mechanism of Action Ergotamine acts as an agonist at 5-HT2 receptors, causing vasoconstriction. (U199, U200, S918)
Target 9 Description 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 9 Synonyms
  1. 5-HTR2C; 5-HT-2C; 5-HT2C; 5HT-1C; Serotonin receptor 2C
Target 9 Gene Name HTR2C
Target 9 Protein Sequence >5-hydroxytryptamine receptor 2C 
MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI
VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW
PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA
ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV
LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM
QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC
SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN
EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
Target 9 Number of Residues 458
Target 9 Molecular Weight 51820.7
Target 9 Theoretical pI 9.11
Target 9 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 9 General Function Involved in protein binding
Target 9 Pathways Not Available
Target 9 Reactions Not Available
Target 9 Signals
  • None
Target 9 Transmembrane Regions
  • 53-78
  • 90-110
  • 128-150
  • 171-193
  • 214-235
  • 312-333
  • 349-371
Target 9 Essentiality Non Essential
Target 9 Domain Function PF00001:7tm_1
Target 9 GenBank ID Protein Not Available
Target 9 UniProtKB ID P28335 Link Image
Target 9 Cellular Location Cell membrane
Target 9 Gene Sequence >1377 bp 
ATGGTGAACCTGAGGAATGCGGTGCATTCATTCCTTGTGCACCTAATTGGCCTATTGGTT
TGGCAATGTGATATTTCTGTGAGCCCAGTAGCAGCTATAGTAACTGACATTTTCAATACC
TCCGATGGTGGACGCTTCAAATTCCCAGACGGGGTACAAAACTGGCCAGCACTTTCAATC
GTCATCATAATAATCATGACAATAGGTGGCAACATCCTTGTGATCATGGCAGTAAGCATG
GAAAAGAAACTGCACAATGCCACCAATTACTTCTTAATGTCCCTAGCCATTGCTGATATG
CTAGTGGGACTACTTGTCATGCCCCTGTCTCTCCTGGCAATCCTTTATGATTATGTCTGG
CCACTACCTAGATATTTGTGCCCCGTCTGGATTTCTTTAGATGTTTTATTTTCAACAGCG
TCCATCATGCACCTCTGCGCTATATCGCTGGATCGGTATGTAGCAATACGTAATCCTATT
GAGCATAGCCGTTTCAATTCGCGGACTAAGGCCATCATGAAGATTGCTATTGTTTGGGCA
ATTTCTATAGGTGTATCAGTTCCTATCCCTGTGATTGGACTGAGGGACGAAGAAAAGGTG
TTCGTGAACAACACGACGTGCGTGCTCAACGACCCAAATTTCGTTCTTATTGGGTCCTTC
GTAGCTTTCTTCATACCGCTGACGATTATGGTGATTACGTATTGCCTGACCATCTACGTT
CTGCGCCGACAAGCTTTGATGTTACTGCACGGCCACACCGAGGAACCGCCTGGACTAAGT
CTGGATTTCCTGAAGTGCTGCAAGAGGAATACGGCCGAGGAAGAGAACTCTGCAAACCCT
AACCAAGACCAGAACGCACGCCGAAGAAAGAAGAAGGAGAGACGTCCTAGGGGCACCATG
CAGGCTATCAACAATGAAAGAAAAGCTTCGAAAGTCCTTGGGATTGTTTTCTTTGTGTTT
CTGATCATGTGGTGCCCATTTTTCATTACCAATATTCTGTCTGTTCTTTGTGAGAAGTCC
TGTAACCAAAAGCTCATGGAAAAGCTTCTGAATGTGTTTGTTTGGATTGGCTATGTTTGT
TCAGGAATCAATCCTCTGGTGTATACTCTGTTCAACAAAATTTACCGAAGGGCATTCTCC
AACTATTTGCGTTGCAATTATAAGGTAGAGAAAAAGCCTCCTGTCAGGCAGATTCCAAGA
GTTGCCGCCACTGCTTTGTCTGGGAGGGAGCTTAATGTTAACATTTATCGGCATACCAAT
GAACCGGTGATCGAGAAAGCCAGTGACAATGAGCCCGGTATAGAGATGCAAGTTGAGAAT
TTAGAGTTACCAGTAAATCCCTCCAGTGTGGTTAGCGAAAGGATTAGCAGTGTGTGA
Target 9 GenBank Gene ID Not Available
Target 9 GeneCard ID HTR2C Link Image
Target 9 GenAtlas ID HTR2C Link Image
Target 9 HGNC ID HGNC:5295 Link Image
Target 9 Chromosome Location Not Available
Target 9 Locus Xq24
Target 9 SNPs SNPJam Report Link Image
Target 9 Toxin References
  • S918 - Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  • U200 - Panconesi A, Anselmi B, Curradi C, Perfetto F, Piluso A, Franchi G: Comparison between venoconstrictor effects of sumatriptan and ergotamine in migraine patients. Headache. 1994 Apr;34(4):194-7. [PubMed Link Image]
  • U199 - Bom AH, Heiligers JP, Saxena PR, Verdouw PD: Reduction of cephalic arteriovenous shunting by ergotamine is not mediated by 5-HT1-like or 5-HT2 receptors. Br J Pharmacol. 1989 Jun;97(2):383-90. [PubMed Link Image]
Target 9 General References 1722404; 7895773; 8812491; 9928237; 15772651; 15489334; 11150294; 7557992; 10206230
Target 10 [top]
Target 10 ID 1193
Target 10 Name Alpha-1B adrenergic receptor
Target 10 Mechanism of Action Ergotamine acts as an agonist at alpha-adrenergic receptors, causing vasoconstriction. (U198)
Target 10 Description This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system
Target 10 Synonyms
  1. Alpha 1B-adrenoreceptor; Alpha 1B-adrenoceptor
Target 10 Gene Name ADRA1B
Target 10 Protein Sequence >Alpha-1B adrenergic receptor 
MNPDLDTGHNTSAPAHWGELKNANFTGPNQTSSNSTLPQLDITRAISVGLVLGAFILFAI
VGNILVILSVACNRHLRTPTNYFIVNLAMADLLLSFTVLPFSAALEVLGYWVLGRIFCDI
WAAVDVLCCTASILSLCAISIDRYIGVRYSLQYPTLVTRRKAILALLSVWVLSTVISIGP
LLGWKEPAPNDDKECGVTEEPFYALFSSLGSFYIPLAVILVMYCRVYIVAKRTTKNLEAG
VMKEMSNSKELTLRIHSKNFHEDTLSSTKAKGHNPRSSIAVKLFKFSREKKAAKTLGIVV
GMFILCWLPFFIALPLGSLFSTLKPPDAVFKVVFWLGYFNSCLNPIIYPCSSKEFKRAFV
RILGCQCRGRGRRRRRRRRRLGGCAYTYRPWTRGGSLERSQSRKDSLDDSGSCLSGSQRT
LPSASPSPGYLGRGAPPPVELCAFPEWKAPGALLSLPAPEPPGRRGRHDSGPLFTFKLLT
EPESPGTDGGASNGGCEAAADVANGQPGFKSNMPLAPGQF
Target 10 Number of Residues 520
Target 10 Molecular Weight 56835.4
Target 10 Theoretical pI 9.79
Target 10 GO Classification
Function
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-adrenergic receptor activity
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 10 General Function Involved in alpha1-adrenergic receptor activity
Target 10 Pathways Not Available
Target 10 Reactions Not Available
Target 10 Signals
  • None
Target 10 Transmembrane Regions
  • 46-70
  • 84-105
  • 116-141
  • 162-184
  • 202-224
  • 296-319
  • 327-351
Target 10 Essentiality Non Essential
Target 10 Domain Function PF00001:7tm_1
Target 10 GenBank ID Protein Not Available
Target 10 UniProtKB ID P35368 Link Image
Target 10 Cellular Location Cell membrane
Target 10 Gene Sequence >1563 bp 
ATGAATCCCGACCTGGACACCGGCCACAACACATCAGCACCTGCCCACTGGGGAGAGTTG
AAAAATGCCAACTTCACTGGCCCCAACCAGACCTCGAGCAACTCCACACTGCCCCAGCTG
GACATCACCAGGGCCATCTCTGTGGGCCTGGTGCTGGGCGCCTTCATCCTCTTTGCCATC
GTGGGCAACATCCTAGTCATCTTGTCTGTGGCCTGCAACCGGCACCTGCGGACGCCCACC
AACTACTTCATTGTCAACCTGGCCATGGCCGACCTGCTGTTGAGCTTCACCGTCCTGCCC
TTCTCAGCGGCCCTAGAGGTGCTCGGCTACTGGGTGCTGGGGCGGATCTTCTGTGACATC
TGGGCAGCCGTGGATGTCCTGTGCTGCACAGCGTCCATTCTGAGCCTGTGCGCCATCTCC
ATCGATCGCTACATCGGGGTGCGCTACTCTCTGCAGTATCCCACGCTGGTCACCCGGAGG
AAGGCCATCTTGGCGCTGCTCAGTGTCTGGGTCTTGTCCACCGTCATCTCCATCGGGCCT
CTCCTTGGGTGGAAGGAGCCGGCACCCAACGATGACAAGGAGTGCGGGGTCACCGAAGAA
CCCTTCTATGCCCTCTTCTCCTCTCTGGGCTCCTTCTACATCCCTCTGGCGGTCATTCTA
GTCATGTACTGCCGTGTCTATATAGTGGCCAAGAGAACCACCAAGAACCTAGAGGCAGGA
GTCATGAAGGAGATGTCCAACTCCAAGGAGCTGACCCTGAGGATCCATTCCAAGAACTTT
CACGAGGACACCCTTAGCAGTACCAAGGCCAAGGGCCACAACCCCAGGAGTTCCATAGCT
GTCAAACTTTTTAAGTTCTCCAGGGAAAAGAAAGCAGCTAAGACGTTGGGCATTGTGGTC
GGTATGTTCATCTTGTGCTGGCTACCCTTCTTCATCGCTCTACCGCTTGGCTCCTTGTTC
TCCACCCTGAAGCCCCCCGACGCCGTGTTCAAGGTGGTGTTCTGGCTGGGCTACTTCAAC
AGCTGCCTCAACCCCATCATCTACCCATGCTCCAGCAAGGAGTTCAAGCGCGCTTTCGTG
CGCATCCTCGGGTGCCAGTGCCGCGGCCGCGGCCGCCGCCGACGCCGCCGCCGCCGTCGC
CTGGGCGGCTGCGCCTACACCTACCGGCCGTGGACGCGCGGCGGCTCGCTGGAGCGCTCG
CAGTCGCGCAAGGACTCGCTGGACGACAGCGGCAGCTGCCTGAGCGGCAGCCAGCGGACC
CTGCCCTCGGCCTCGCCGAGCCCGGGCTACCTGGGCCGCGGCGCGCCACCGCCAGTCGAG
CTGTGCGCCTTCCCCGAGTGGAAGGCGCCCGGCGCCCTCCTGAGCCTGCCCGCGCCTGAG
CCCCCCGGCCGCCGCGGCCGCCACGACTCGGGCCCGCTCTTCACCTTCAAGCTCCTGACC
GAGCCCGAGAGCCCCGGGACCGACGGCGGCGCCAGCAACGGAGGCTGCGAGGCCGCGGCC
GACGTGGCCAACGGGCAGCCGGGCTTCAAAAGCAACATGCCCCTGGCGCCCGGGCAGTTT
TAG
Target 10 GenBank Gene ID Not Available
Target 10 GeneCard ID ADRA1B Link Image
Target 10 GenAtlas ID ADRA1B Link Image
Target 10 HGNC ID HGNC:278 Link Image
Target 10 Chromosome Location Not Available
Target 10 Locus 5q23-q32
Target 10 SNPs SNPJam Report Link Image
Target 10 Toxin References
  • U198 - Valdivia LF, Centurion D, Arulmani U, Saxena PR, Villalon CM: 5-HT1B receptors, alpha2A/2C- and, to a lesser extent, alpha1-adrenoceptors mediate the external carotid vasoconstriction to ergotamine in vagosympathectomised dogs. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):46-53. Epub 2004 Jun 29. [PubMed Link Image]
  • W738 - Görnemann T, Jähnichen S, Schurad B, Latté KP, Horowski R, Tack J, Flieger M, Pertz HH. Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jan;376(5):321-30. Epub 2007 Dec 8. [PubMed Link Image]
Target 10 General References 1328250; 8183249; 7815325
Target 11 [top]
Target 11 ID 1203
Target 11 Name Alpha-1D adrenergic receptor
Target 11 Mechanism of Action Ergotamine acts as an agonist at alpha-adrenergic receptors, causing vasoconstriction. (U198)
Target 11 Description This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium
Target 11 Synonyms
  1. Alpha 1D-adrenoreceptor; Alpha 1D-adrenoceptor; Alpha-1A adrenergic receptor; Alpha-adrenergic receptor 1a
Target 11 Gene Name ADRA1D
Target 11 Protein Sequence >Alpha-1D adrenergic receptor 
MTFRDLLSVSFEGPRPDSSAGGSSAGGGGGSAGGAAPSEGPAVGGVPGGAGGGGGVVGAG
SGEDNRSSAGEPGSAGAGGDVNGTAAVGGLVVSAQGVGVGVFLAAFILMAVAGNLLVILS
VACNRHLQTVTNYFIVNLAVADLLLSATVLPFSATMEVLGFWAFGRAFCDVWAAVDVLCC
TASILSLCTISVDRYVGVRHSLKYPAIMTERKAAAILALLWVVALVVSVGPLLGWKEPVP
PDERFCGITEEAGYAVFSSVCSFYLPMAVIVVMYCRVYVVARSTTRSLEAGVKRERGKAS
EVVLRIHCRGAATGADGAHGMRSAKGHTFRSSLSVRLLKFSREKKAAKTLAIVVGVFVLC
WFPFFFVLPLGSLFPQLKPSEGVFKVIFWLGYFNSCVNPLIYPCSSREFKRAFLRLLRCQ
CRRRRRRRPLWRVYGHHWRASTSGLRQDCAPSSGDAPPGAPLALTALPDPDPEPPGTPEM
QAPVASRRKPPSAFREWRLLGPFRRPTTQLRAKVSSLSHKIRAGGAQRAEAACAQRSEVE
AVSLGVPHEVAEGATCQAYELADYSNLRETDI
Target 11 Number of Residues 572
Target 11 Molecular Weight 60462.2
Target 11 Theoretical pI 9.44
Target 11 GO Classification
Function
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-adrenergic receptor activity
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 11 General Function Carbohydrate transport and metabolism
Target 11 Pathways Not Available
Target 11 Reactions Not Available
Target 11 Signals
  • None
Target 11 Transmembrane Regions
  • 96-121
  • 134-159
  • 170-192
  • 214-238
  • 252-275
  • 349-373
  • 381-405
Target 11 Essentiality Non Essential
Target 11 Domain Function PF00001:7tm_1
Target 11 GenBank ID Protein Not Available
Target 11 UniProtKB ID P25100 Link Image
Target 11 Cellular Location Cell membrane
Target 11 Gene Sequence >1506 bp 
ATGGCGGCCGCCTTGCGCTCGGTCATGATGGCTGGGTACTTGAGTGAGTGGCGCACGCCC
ACGTACCGGTCCACGGAGATGGTGCAGAGGCTGAGGATGGAGGCCGTGCAGCACAGCACG
TCCACGGCGGCCGTCGGGGGACTGGTGGTGAGCGCGCAGGGCGTGGGCGTGGGCGTCTTC
CTGGCAGCCTTCATCCTTATGGCCGTGGCAGGTAACCTGCTTGTCATCCTCTCAGTGGCC
TGCAACCGCCACCTGCAGACCGTCACCAACTATTTCATCGTGAACCTGGCCGTGGCCGAC
CTGCTGCTGAGCGCCACCGTACTGCCCTTCTCGGCCACCATGGAGGTTCTGGGCTTCTGG
GCCTTTGGCCGCGCCTTCTGCGACGTATGGGCCGCCGTGGACGTGCTGTGCTGCACGGCC
TCCATCCTCAGCCTCTGCACCATCTCCGTGGACCGGTACGTGGGCGTGCGCCACTCACTC
AAGTACCCAGCCATCATGACCGAGCGCAAGGCGGCCGCCATCCTGGCCCTGCTCTGGGTC
GTAGCCCTGGTGGTGTCCGTAGGGCCCCTGCTGGGCTGGAAGGAGCCCGTGCCCCCTGAC
GAGCGCTTCTGCGGTATCACCGAGGAGGCGGGCTACGCTGTCTTCTCCTCCGTGTGCTCC
TTCTACCTGCCCATGGCGGTCATCGTGGTCATGTACTGCCGCGTGTACGTGGTCGCGCGC
AGCACCACGCGCAGCCTCGAGGCAGGCGTCAAGCGCGAGCGAGGCAAGGCCTCCGAGGTG
GTGCTGCGCATCCACTGTCGCGGCGCGGCCACGGGCGCCGACGGGGCGCACGGCATGCGC
AGCGCCAAGGGCCACACCTTCCGCAGCTCGCTCTCCGTGCGCCTGCTCAAGTTCTCCCGT
GAGAAGAAAGCGGCCAAGACTCTGGCCATCGTCGTGGGTGTCTTCGTGCTCTGCTGGTTC
CCTTTCTTCTTTGTCCTGCCGCTCGGCTCCTTGTTCCCGCAGCTGAAGCCATCGGAGGGC
GTCTTCAAGGTCATCTTCTGGCTCGGCTACTTCAACAGCTGCGTGAACCCGCTCATCTAC
CCCTGTTCCAGCCGCGAGTTCAAGCGCGCCTTCCTCCGTCTCCTGCGCTGCCAGTGCCGT
CGTCGCCGGCGCCGCCGCCCTCTCTGGCGTGTCTACGGCCACCACTGGCGGGCCTCCACC
AGCGGCCTGCGCCAGGACTGCGCCCCGAGTTCGGGCGACGCGCCCCCCGGAGCGCCGCTG
GCCCTCACCGCGCTCCCCGACCCCGACCCCGAACCCCCAGGCACGCCCGAGATGCAGGCT
CCGGTCGCCAGCCGTCGAAGCCACCCAGCGCCTTCCGCGAGTGGAGGCTGCTGGGGCCGT
TCCGGAGACCCACGACCCAGCTGCGCGCCAAAGTCTCCAGCCTGTCGCACAAGATCGCCG
CCGGGGGCGCGCAGCGCGCAGAGGCAGCGTGCGCCCAGCGCTCAGAGGTGGAGGCTGTGT
CCCTAG
Target 11 GenBank Gene ID Not Available
Target 11 GeneCard ID ADRA1D Link Image
Target 11 GenAtlas ID ADRA1D Link Image
Target 11 HGNC ID HGNC:280 Link Image
Target 11 Chromosome Location Chromosome:20
Target 11 Locus 20p13
Target 11 SNPs SNPJam Report Link Image
Target 11 Toxin References
  • U198 - Valdivia LF, Centurion D, Arulmani U, Saxena PR, Villalon CM: 5-HT1B receptors, alpha2A/2C- and, to a lesser extent, alpha1-adrenoceptors mediate the external carotid vasoconstriction to ergotamine in vagosympathectomised dogs. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):46-53. Epub 2004 Jun 29. [PubMed Link Image]
  • W738 - Görnemann T, Jähnichen S, Schurad B, Latté KP, Horowski R, Tack J, Flieger M, Pertz HH. Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jan;376(5):321-30. Epub 2007 Dec 8. [PubMed Link Image]
Target 11 General References 1656955; 8183249; 7815325; 8024574; 7746284; 11780052
Target 12 [top]
Target 12 ID 1367
Target 12 Name Alpha-2C adrenergic receptor
Target 12 Mechanism of Action Ergotamine acts as an agonist at alpha-adrenergic receptors, causing vasoconstriction. (U198)
Target 12 Description Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins
Target 12 Synonyms
  1. Alpha-2C adrenoreceptor; Alpha-2C adrenoceptor; Alpha-2 adrenergic receptor subtype C4
Target 12 Gene Name ADRA2C
Target 12 Protein Sequence >Alpha-2C adrenergic receptor 
MASPALAAALAVAAAAGPNASGAGERGSGGVANASGASWGPPRGQYSAGAVAGLAAVVGF
LIVFTVVGNVLVVIAVLTSRALRAPQNLFLVSLASADILVATLVMPFSLANELMAYWYFG
QVWCGVYLALDVLFCTSSIVHLCAISLDRYWSVTQAVEYNLKRTPRRVKATIVAVWLISA
VISFPPLVSLYRQPDGAAYPQCGLNDETWYILSSCIGSFFAPCLIMGLVYARIYRVAKLR
TRTLSEKRAPVGPDGASPTTENGLGAAAGAGENGHCAPPPADVEPDESSAAAERRRRRGA
LRRGGRRRAGAEGGAGGADGQGAGPGAAESGALTASRSPGPGGRLSRASSRSVEFFLSRR
RRARSSVCRRKVAQAREKRFTFVLAVVMGVFVLCWFPFFFSYSLYGICREACQVPGPLFK
FFFWIGYCNSSLNPVIYTVFNQDFRRSFKHILFRRRRRGFRQ
Target 12 Number of Residues 462
Target 12 Molecular Weight 49521.6
Target 12 Theoretical pI 10.69
Target 12 GO Classification
Function
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha2-adrenergic receptor activity
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 12 General Function Involved in alpha2-adrenergic receptor activity
Target 12 Pathways Not Available
Target 12 Reactions Not Available
Target 12 Signals
  • None
Target 12 Transmembrane Regions
  • 52-76
  • 89-114
  • 125-147
  • 169-191
  • 208-231
  • 380-407
  • 421-441
Target 12 Essentiality Non Essential
Target 12 Domain Function PF00001:7tm_1
Target 12 GenBank ID Protein Not Available
Target 12 UniProtKB ID P18825 Link Image
Target 12 Cellular Location Cell membrane
Target 12 Gene Sequence >1386 bp 
ATGGCGTCCCCGGCGCTGGCGGCGGCGCTGGCGGTGGCGGCAGCGGCGGGCCCCAATGCG
AGCGGCGCGGGCGAGAGGGGCAGCGGCGGGGTTGCCAATGCCTCGGGGGCTTCCTGGGGG
CCGCCGCGCGGCCAGTACTCGGCGGGCGCGGTGGCAGGGCTGGCTGCCGTGGTGGGCTTC
CTCATCGTCTTCACCGTGGTGGGCAACGTGCTGGTGGTGATCGCCGTGCTGACCAGCCGG
GCGCTGCGCGCGCCACAGAACCTCTTCCTGGTGTCGCTGGCCTCGGCCGACATCCTGGTG
GCCACGCTGGTCATGCCCTTCTCGTTGGCCAACGAGCTCATGGCCTACTGGTACTTCGGG
CAGGTGTGGTGCGGCGTGTACCTGGCGCTCGATGTGCTGTTTTGCACCTCGTCGATCGTG
CATCTGTGTGCCATCAGCCTGGACCGCTACTGGTCGGTGACGCAGGCCGTCGAGTACAAC
CTGAAGCGCACACCACGCCGCGTCAAGGCCACCATCGTCGCCGTGTGGCTCATCTCGGCC
GTCATCTCCTTCCCGCCGCTGGTCTCGCTCTACCGCCAGCCCGACGGCGCCGCCTACCCG
CAGTGCGGCCTCAACGACGAGACCTGGTACATCCTGTCCTCCTGCATCGGCTCCTTCTTC
GCGCCCTGCCTCATCATGGGCCTGGTCTACGCGCGCATCTACCGAGTGGCCAAGCGTCGC
ACGCGCACGCTCAGCGAGAAGCGCGCCCCCGTGGGCCCCGACGGTGCGTCCCCGACTACC
GAAAACGGGCTGGGCGCGGCGGCAGGCGAGGCGAGAACGGGCACTGCGCGCCCCCGCCCG
CCGACGTGGAGCCGGACGAGAGCAGCGCAGCGGCCGAGAGGCGGCGCGCCGGGGCCGTTG
CGGCGGGGCGGGCGGCGGCGAGCGGGCGCGGAGGGGGGCGCGGGCGGTGCGGACGGGCAG
GGGGCGGGGCCGGGGGCGGCTCAGTCGGGGGCGCTGACCGCCTCCAGGTCCCCGGGGCCC
GGTGGCCGCCTCTCGCGCGCCAGCTCGCGCTCCGTCGAGTTCTTCCTGTCGCGCCGGCGC
CGGGCGCGCAGCAGCGTGTGCCGCCGCAAGGTGGCCCAGGCGCGCGAGAAGCGCTTCACC
TTTGTGCTGGCTGTGGTCATGGGCGTGTTCGTGCTCTGCTGGTTCCCCTTCTTCTTCATC
TACAGCCTGTACGGCATCTGCCGCGAGGCCTGCCAGGTGCCCGGCCCGCTCTTCAAGTTC
TTCTTCTGGATCGGCTACTGCAACAGCTCGCTCAACCCGGTCATCTACACGGTCTTCAAC
CAGGATTTCCGGCCATCCTTCAAGCACATCCTCTTCCGACGGAGGAGAAGGGGCTTCAGG
CAGTGA
Target 12 GenBank Gene ID Not Available
Target 12 GeneCard ID ADRA2C Link Image
Target 12 GenAtlas ID ADRA2C Link Image
Target 12 HGNC ID HGNC:283 Link Image
Target 12 Chromosome Location Not Available
Target 12 Locus 4p16
Target 12 SNPs SNPJam Report Link Image
Target 12 Toxin References
  • U198 - Valdivia LF, Centurion D, Arulmani U, Saxena PR, Villalon CM: 5-HT1B receptors, alpha2A/2C- and, to a lesser extent, alpha1-adrenoceptors mediate the external carotid vasoconstriction to ergotamine in vagosympathectomised dogs. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):46-53. Epub 2004 Jun 29. [PubMed Link Image]
Target 12 General References 2842764; 9371698; 10801795; 15319474; 1849485

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.