Drugbank Logo

Showing drug card for Methysergide (DB00247)

Legend: drug field target field enzyme field

for drugs
Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:06:58
Primary Accession Number DB00247
Secondary Accession Number
  • APRD00463
Name Methysergide
Drug Type
  • Approved
  • Small Molecule
Description An ergot derivative that is a congener of lysergic acid diethylamide. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome. [PubChem]
Synonyms
  1. Methyllysergic acid butanolamide
  2. Methysergid
  3. Methysergidum [INN-Latin]
  4. Metisergide [DCIT]
  5. Metisergido [INN-Spanish]
  6. N-(1-(Hydroxymethyl)propyl)-1-methyl-dextro-(+)-lysergamide
  7. N-(alpha-(Hydroxymethyl)propyl)-1-methyl-dextro-lysergamide
Brand Names
  1. Deseril
  2. Desernil
  3. Desernyl
  4. Deseryl
  5. Sansert
Brand Mixtures Not Available
Chemical IUPAC Name Not Available
Chemical Formula C21H27N3O2
Chemical Structure Structure
CAS Registry Number 361-37-5
InChI Identifier InChI=1/C21H27N3O2/c1-4-15(12-25)22-21(26)14-8-17-16-6-5-7-18-20(16)13(10-23(18)2)9-19(17)24(3)11-14/h5-8,10,14-15,19,25H,4,9,11-12H2,1-3H3,(H,22,26)/t14-,15+,19-/m1/s1/f/h22H
InChI Key KPJZHOPZRAFDTN-YBSCGTCVDI
KEGG Drug D02357 Link Image
KEGG Compound C07199 Link Image
PubChem Compound 9681 Link Image
PubChem Substance 7849416 Link Image
ChEBI ID Not Available
PharmGKB ID PA450471 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 00027499 Link Image
RxList Link http://www.rxlist.com/cgi/generic3/sansert.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Methysergide Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS) Not Available
Synthesis Reference Not Available
Average Molecular Weight 353.4580
Monoisotopic Molecular Weight 353.2103
State Solid
Melting Point 195 oC
Experimental Water Solubility Not Available Source: PhysProp
Predicted Water Solubility 2.24e-01 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 1.5 Source: PhysProp
Predicted LogP 2.22 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -3.20 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 CC[C@@H](CO)NC(=O)[C@H]1CN(C)[C@@H]2CC3=CN(C)C4=CC=CC(C2=C1)=C34
Canonical SMILES CCC(CO)NC(=O)C1CN(C)C2CC3=CN(C)C4=CC=CC(C2=C1)=C34
Drug Category
  • Serotonin Antagonists
  • Sympatholytics
  • Vasoconstrictor Agents
ATC Codes
AHFS Codes
  • 12:16.00
Indication For the treatment of vascular headache
Pharmacology Methysergide has been shown, in vitro and in vivo, to inhibit or block the effects of serotonin, a substance which may be involved in the mechanism of vascular headaches. Serotonin has been variously described as a central neurohumoral agent or chemical mediator, as a "headache substance" acting directly or indirectly to lower pain threshold, as an intrinsic "motor hormone" of the gastrointestinal tract, and as a "hormone" involved in connective tissue reparative processes.
Mechanism of Action Methysergide is serotonin antagonists acts on central nervous system (CNS), which directly stimulates the smooth muscle leading to vasoconstriction. Some alpha-adrenergic blocking activity has been reported. Suggestions have been made by investigators as to the mechanism whereby Methysergide produces its clinical effects, but this has not been finally established, although it may be related to the antiserotonin effect.
Absorption Rapid
Toxicity Few cases of acute methysergide intoxication have been reported. The possible symptom complex is therefore not fully known. The following symptoms are based on these few case reports. Euphoria, hyperactivity, tachycardia, dilated pupils, and dizziness have been reported in a child with a dose of 20-24 mg of methysergide. In adults, peripheral vasospasm, with diminished or absent pulses, coldness, mottling and cyanosis, has been observed at a dose of 200 mg. Ischemic tissue damage has not been reported in acute overdosage with methysergide.
Protein Binding Not Available
Biotransformation Hepatic
Half Life Not Available
Dosage Forms
Form Route
Tablet Oral
Patient Information Not Available
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Acebutolol Ischemia with risk of gangrene
Almotriptan Possible severe and prolonged vasoconstriction
Amyl Nitrite Possible antagonism of action
Atenolol Ischemia with risk of gangrene
Betaxolol Ischemia with risk of gangrene
Bevantolol Ischemia with risk of gangrene
Bisoprolol Ischemia with risk of gangrene
Carteolol Ischemia with risk of gangrene
Carvedilol Ischemia with risk of gangrene
Clarithromycin Risk of ergotism and severe ischemia with this association
Delavirdine The antiretroviral agent may increase the ergot derivative toxicity
Efavirenz The antiretroviral agent may increase the ergot derivative toxicity
Eletriptan Possible severe and prolonged vasoconstriction
Erythrityl Tetranitrate Possible antagonism of action
Erythromycin Possible ergotism and severe ischemia with this combination
Esmolol Ischemia with risk of gangrene
Frovatriptan Possible severe and prolonged vasoconstriction
Isosorbide Dinitrate Possible antagonism of action
Isosorbide Mononitrate Possible antagonism of action
Josamycin Possible ergotism and severe ischemia with this combination
Labetalol Ischemia with risk of gangrene
Metoprolol Ischemia with risk of gangrene
Nadolol Ischemia with risk of gangrene
Naratriptan Possible severe and prolonged vasoconstriction
Nitroglycerin Possible antagonism of action
Oxprenolol Ischemia with risk of gangrene
Penbutolol Ischemia with risk of gangrene
Pindolol Ischemia with risk of gangrene
Posaconazole Contraindicated co-administration
Practolol Ischemia with risk of gangrene
Propranolol Ischemia with risk of gangrene
Rizatriptan Possible severe and prolonged vasoconstriction
Sibutramine Possible serotoninergic syndrome
Sotalol Ischemia with risk of gangrene
Sumatriptan Possible severe and prolonged vasoconstriction
Telithromycin Risk of ergotism and severe ischemia with this association
Timolol Ischemia with risk of gangrene
Troleandomycin Possible ergotism and severe ischemia with this combination
Zolmitriptan Possible severe and prolonged vasoconstriction
Food Interactions
  • Take with food to reduce irritation.
Pathways Not Available
General References
  1. Drugs.com Link Image
  2. Wikipedia Link Image
  3. RxList Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. 5-hydroxytryptamine 1A receptor
  2. 5-hydroxytryptamine 2A receptor
  3. 5-hydroxytryptamine 2C receptor
  4. 5-hydroxytryptamine 7 receptor
Drug Target 1 [top]
Target 1 ID 320
Target 1 Name 5-hydroxytryptamine 1A receptor
Target 1 Synonyms
  1. 5- HT1A
  2. 5-HT-1A
  3. G-21
  4. Serotonin receptor 1A
Target 1 Gene Name HTR1A
Target 1 Protein Sequence >5-hydroxytryptamine 1A receptor 
MDVLSPGQGNNTTSPPAPFETGGNTTGISDVTVSYQVITSLLLGTLIFCAVLGNACVVAA
IALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCC
TSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPED
RSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVKKVEKTGADT
RHGASPAPQPKKSVNGESGSRNWRLGVESKAGGALCANGAVRQGDDGAALEVIEVHRVGN
SKEHLPLPSEAGPTPCAPASFERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLP
FFIVALVLPFCESSCHMPTLLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFC
RQ
Target 1 Number of Residues 429
Target 1 Molecular Weight 46107
Target 1 Theoretical pI 9.05
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. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 37-62
  • 74-98
  • 110-132
  • 153-178
  • 192-217
  • 346-367
  • 379-403
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 189928 Link Image
Target 1 UniProtKB/Swiss-Prot ID P08908 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name 5HT1A_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >1266 bp 
ATGGATGTGCTCAGCCCTGGTCAGGGCAACAACACCACATCACCACCGGCTCCCTTTGAG
ACCGGCGGCAACACTACTGGTATCTCCGACGTGACCGTCAGCTACCAAGTGATCACCTCT
CTGCTGCTGGGCACGCTCATCTTCTGCGCGGTGCTGGGCAATGCGTGCGTGGTGGCTGCC
ATCGCCTTGGAGCGCTCCCTGCAGAACGTGGCCAATTATCTTATTGGCTCTTTGGCGGTC
ACCGACCTCATGGTGTCGGTGTTGGTGCTGCCCATGGCCGCGCTGTATCAGGTGCTCAAC
AAGTGGACACTGGGCCAGGTAACCTGCGACCTGTTCATCGCCCTCGACGTGCTGTGCTGC
ACCTCATCCATCTTGCACCTGTGCGCCATCGCGCTGGACAGGTACTGGGCCATCACGGAC
CCCATCGACTACGTGAACAAGAGGACGCCCCGGCCGCGTGCGCTCATCTCGCTCACTTGG
CTTATTGGCTTCCTCATCTCTATCCCGCCCATCCTGGGCTGGCGCACCCCGGAAGACCGC
TCGGACCCCGACGCATGCACCATTAGCAAGGATCATGGCTACACTATCTATTCCACCTTT
GGAGCTTTCTACATCCCGCTGCTGCTCATGCTGGTTCTCTATGGGCGCATATTCCGAGCT
GCGCGCTTCCGCATCCGCAAGACGGTCAAAAAGGTGGAGAAGACCGGAGCGGACACCCGC
CATGGAGCATCTCCCGCCCCGCAGCCCAAGAAGAGTGTGAATGGAGAGTCGGGGAGCAGG
AACTGGAGGCTGGGCGTGGAGAGCAAGGCTGGGGGTGCTCTGTGCGCCAATGGCGCGGTG
AGGCAAGGTGACGATGGCGCCGCCCTGGAGGTGATCGAGGTGCACCGAGTGGGCAACTCC
AAAGAGCACTTGCCTCTGCCCAGCGAGGCTGGTCCTACCCCTTGTGCCCCCGCCTCTTTC
GAGAGGAAAAATGAGCGCAACGCCGAGGCGAAGCGCAAGATGGCCCTGGCCCGAGAGAGG
AAGACAGTGAAGACGCTGGGCATCATCATGGGCACCTTCATCCTCTGCTGGCTGCCCTTC
TTCATCGTGGCTCTTGTTCTGCCCTTCTGCGAGAGCAGCTGCCACATGCCCACCCTGTTG
GGCGCCATAATCAATTGGCTGGGCTACTCCAACTCTCTGCTTAACCCCGTCATTTACGCA
TACTTCAACAAGGACTTTCAAAACGCGTTTAAGAAGATCATTAAGTGTAACTTCTGCCGC
CAGTGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID HTR1A Link Image
Target 1 GenAtlas ID HTR1A Link Image
Target 1 HGNC ID HGNC:5286 Link Image
Target 1 Chromosome Location 5
Target 1 Locus 5q11.2-q13
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Parks CL, Chang LS, Shenk T: A polymerase chain reaction mediated by a single primer: cloning of genomic sequences adjacent to a serotonin receptor protein coding region. Nucleic Acids Res. 1991 Dec;19(25):7155-60. [PubMed Link Image]
  2. Kobilka BK, Frielle T, Collins S, Yang-Feng T, Kobilka TS, Francke U, Lefkowitz RJ, Caron MG: An intronless gene encoding a potential member of the family of receptors coupled to guanine nucleotide regulatory proteins. Nature. 1987 Sep 3-9;329(6134):75-9. [PubMed Link Image]
  3. Fargin A, Raymond JR, Lohse MJ, Kobilka BK, Caron MG, Lefkowitz RJ: The genomic clone G-21 which resembles a beta-adrenergic receptor sequence encodes the 5-HT1A receptor. Nature. 1988 Sep 22;335(6188):358-60. [PubMed Link Image]
  4. Nakhai B, Nielsen DA, Linnoila M, Goldman D: Two naturally occurring amino acid substitutions in the human 5-HT1A receptor: glycine 22 to serine 22 and isoleucine 28 to valine 28. Biochem Biophys Res Commun. 1995 May 16;210(2):530-6. [PubMed Link Image]
  5. Aune TM, McGrath KM, Sarr T, Bombara MP, Kelley KA: Expression of 5HT1a receptors on activated human T cells. Regulation of cyclic AMP levels and T cell proliferation by 5-hydroxytryptamine. J Immunol. 1993 Aug 1;151(3):1175-83. [PubMed Link Image]
  6. Kawanishi Y, Harada S, Tachikawa H, Okubo T, Shiraishi H: Novel mutations in the promoter and coding region of the human 5-HT1A receptor gene and association analysis in schizophrenia. Am J Med Genet. 1998 Sep 7;81(5):434-9. [PubMed Link Image]
Target 1 Drug References
  1. Scrogin KE, Johnson AK, Brooks VL: Methysergide delays the decompensatory responses to severe hemorrhage by activating 5-HT(1A) receptors. Am J Physiol Regul Integr Comp Physiol. 2000 Nov;279(5):R1776-86. [PubMed Link Image]
  2. Sugimoto Y, Inoue K, Yamada J: The tricyclic antidepressant clomipramine increases plasma glucose levels of mice. J Pharmacol Sci. 2003 Sep;93(1):74-9. [PubMed Link Image]
  3. Sugimoto Y, Inoue K, Yamada J: Involvement of 5-HT(2) receptor in imipramine-induced hyperglycemia in mice. Horm Metab Res. 2003 Sep;35(9):511-6. [PubMed Link Image]
  4. Skyba DA, Radhakrishnan R, Rohlwing JJ, Wright A, Sluka KA: Joint manipulation reduces hyperalgesia by activation of monoamine receptors but not opioid or GABA receptors in the spinal cord. Pain. 2003 Nov;106(1-2):159-68. [PubMed Link Image]
  5. Pranzatelli MR, Balletti J: Characterization of 5-hydroxytryptamine 1A-like binding sites in human ganglioneuroblastoma. Neurosci Lett. 1991 Oct 28;132(1):117-20. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 502
Target 2 Name 5-hydroxytryptamine 2A receptor
Target 2 Synonyms
  1. 5- HT-2
  2. 5-HT-2A
  3. Serotonin receptor 2A
Target 2 Gene Name HTR2A
Target 2 Protein Sequence >5-hydroxytryptamine 2A receptor 
MDILCEENTSLSSTTNSLMQLNDDTRLYSNDFNSGEANTSDAFNWTVDSENRTNLSCEGC
LSPSCLSLLHLQEKNWSALLTAVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIAD
MLLGFLVMPVSMLTILYGYRWPLPSKLCAVWIYLDVLFSTASIMHLCAISLDRYVAIQNP
IHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSF
VSFFIPLTIMVITYFLTIKSLQKEATLCVSDLGTRAKLASFSFLPQSSLSSEKLFQRSIH
REPGSYTGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNEDVIGA
LLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENKKPLQLILVNTIPALAYK
SSQLQMGQKKNSKQDAKTTDNDCSMVALGKQHSEEASKDNSDGVNEKVSCV
Target 2 Number of Residues 478
Target 2 Molecular Weight 52604
Target 2 Theoretical pI 7.72
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. 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 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 76-99
  • 111-132
  • 148-171
  • 192-215
  • 234-254
  • 325-346
  • 363-384
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 36431 Link Image
Target 2 UniProtKB/Swiss-Prot ID P28223 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name 5HT2A_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Cell membrane
  • multi-pass membrane protein. Localizes to the post-synaptic thickening of axo-dendrit
Target 2 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 2 GenBank Gene ID
Target 2 GeneCard ID HTR2A Link Image
Target 2 GenAtlas ID HTR2A Link Image
Target 2 HGNC ID HGNC:5293 Link Image
Target 2 Chromosome Location 13
Target 2 Locus 13q14-q21
Target 2 SNPs SNPJam Report Link Image
Target 2 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. Marshall SE, Bird TG, Hart K, Welsh KI: Unified approach to the analysis of genetic variation in serotonergic pathways. Am J Med Genet. 1999 Dec 15;88(6):621-7. [PubMed Link Image]
  3. 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]
  4. Chen K, Yang W, Grimsby J, Shih JC: The human 5-HT2 receptor is encoded by a multiple intron-exon gene. Brain Res Mol Brain Res. 1992 Jun;14(1-2):20-6. [PubMed Link Image]
  5. Stam NJ, Van Huizen F, Van Alebeek C, Brands J, Dijkema R, Tonnaer JA, Olijve W: Genomic organization, coding sequence and functional expression of human 5-HT2 and 5-HT1A receptor genes. Eur J Pharmacol. 1992 Oct 1;227(2):153-62. [PubMed Link Image]
  6. Saltzman AG, Morse B, Whitman MM, Ivanshchenko Y, Jaye M, Felder S: Cloning of the human serotonin 5-HT2 and 5-HT1C receptor subtypes. Biochem Biophys Res Commun. 1991 Dec 31;181(3):1469-78. [PubMed Link Image]
  7. Cook EH Jr, Fletcher KE, Wainwright M, Marks N, Yan SY, Leventhal BL: Primary structure of the human platelet serotonin 5-HT2A receptor: identify with frontal cortex serotonin 5-HT2A receptor. J Neurochem. 1994 Aug;63(2):465-9. [PubMed Link Image]
  8. Erdmann J, Shimron-Abarbanell D, Rietschel M, Albus M, Maier W, Korner J, Bondy B, Chen K, Shih JC, Knapp M, Propping P, Nothen MM: Systematic screening for mutations in the human serotonin-2A (5-HT2A) receptor gene: identification of two naturally occurring receptor variants and association analysis in schizophrenia. Hum Genet. 1996 May;97(5):614-9. [PubMed Link Image]
Target 2 Drug References
  1. Castilho VM, Avanzi V, Brandao ML: Antinociception elicited by aversive stimulation of the inferior colliculus. Pharmacol Biochem Behav. 1999 Mar;62(3):425-31. [PubMed Link Image]
  2. Geerts IS, Matthys KE, Herman AG, Bult H: Involvement of 5-HT1B receptors in collar-induced hypersensitivity to 5-hydroxytryptamine of the rabbit carotid artery. Br J Pharmacol. 1999 Jul;127(6):1327-36. [PubMed Link Image]
  3. Shaw AM, Brown C, Irvine J, Bunton DC, MacDonald A: Role of the 5-HT(2A)receptor and alpha(1)-adrenoceptor in the contractile response of rat pulmonary artery to 5-HT in the presence and absence of nitric oxide. Pulm Pharmacol Ther. 2000;13(6):277-85. [PubMed Link Image]
  4. Prins NH, Akkermans LM, Lefebvre RA, Schuurkes JA: Characterization of the receptors involved in the 5-HT-induced excitation of canine antral longitudinal muscle. Br J Pharmacol. 2001 Nov;134(6):1351-9. [PubMed Link Image]
  5. Connor JD, Rasheed H, Gilani AH, Cheema M, Rizvi Z, Saeed SA: Second messengers in platelet aggregation evoked by serotonin and A23187, a calcium ionophore. Life Sci. 2001 Oct 26;69(23):2759-64. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 590
Target 3 Name 5-hydroxytryptamine 2C receptor
Target 3 Synonyms
  1. 5- HT2C
  2. 5-HT-2C
  3. 5-HTR2C
  4. 5HT-1C
  5. Serotonin receptor 2C
Target 3 Gene Name HTR2C
Target 3 Protein Sequence >5-hydroxytryptamine 2C receptor 
MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI
VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW
PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA
ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV
LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM
QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC
SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN
EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
Target 3 Number of Residues 465
Target 3 Molecular Weight 51822
Target 3 Theoretical pI 9.11
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. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 53-78
  • 90-110
  • 128-150
  • 171-193
  • 214-235
  • 312-333
  • 349-371
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 338028 Link Image
Target 3 UniProtKB/Swiss-Prot ID P28335 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name 5HT2C_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 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 3 GenBank Gene ID
Target 3 GeneCard ID HTR2C Link Image
Target 3 GenAtlas ID HTR2C Link Image
Target 3 HGNC ID HGNC:5295 Link Image
Target 3 Chromosome Location X
Target 3 Locus Xq24
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Samochowiec J, Smolka M, Winterer G, Rommelspacher H, Schmidt LG, Sander T: Association analysis between a Cys23Ser substitution polymorphism of the human 5-HT2c receptor gene and neuronal hyperexcitability. Am J Med Genet. 1999 Apr 16;88(2):126-30. [PubMed Link Image]
  2. 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]
  3. Marshall SE, Bird TG, Hart K, Welsh KI: Unified approach to the analysis of genetic variation in serotonergic pathways. Am J Med Genet. 1999 Dec 15;88(6):621-7. [PubMed Link Image]
  4. 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]
  5. Saltzman AG, Morse B, Whitman MM, Ivanshchenko Y, Jaye M, Felder S: Cloning of the human serotonin 5-HT2 and 5-HT1C receptor subtypes. Biochem Biophys Res Commun. 1991 Dec 31;181(3):1469-78. [PubMed Link Image]
  6. Lappalainen J, Zhang L, Dean M, Oz M, Ozaki N, Yu DH, Virkkunen M, Weight F, Linnoila M, Goldman D: Identification, expression, and pharmacology of a Cys23-Ser23 substitution in the human 5-HT2c receptor gene (HTR2C). Genomics. 1995 May 20;27(2):274-9. [PubMed Link Image]
  7. Stam NJ, Vanderheyden P, van Alebeek C, Klomp J, de Boer T, van Delft AM, Olijve W: Genomic organisation and functional expression of the gene encoding the human serotonin 5-HT2C receptor. Eur J Pharmacol. 1994 Nov 15;269(3):339-48. [PubMed Link Image]
  8. Xie E, Zhu L, Zhao L, Chang LS: The human serotonin 5-HT2C receptor: complete cDNA, genomic structure, and alternatively spliced variant. Genomics. 1996 Aug 1;35(3):551-61. [PubMed Link Image]
  9. Niswender CM, Sanders-Bush E, Emeson RB: Identification and characterization of RNA editing events within the 5-HT2C receptor. Ann N Y Acad Sci. 1998 Dec 15;861:38-48. [PubMed Link Image]
Target 3 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 4 [top]
Target 4 ID 716
Target 4 Name 5-hydroxytryptamine 7 receptor
Target 4 Synonyms
  1. 5-HT- X
  2. 5-HT-7
  3. 5HT7
  4. Serotonin receptor 7
Target 4 Gene Name HTR7
Target 4 Protein Sequence >5-hydroxytryptamine 7 receptor 
MMDVNSSGRPDLYGHLRSFLLPEVGRGLPDLSPDGGADPVAGSWAPHLLSEVTASPAPTW
DAPPDNASGCGEQINYGRVEKVVIGSILTLITLLTIAGNCLVVISVCFVKKLRQPSNYLI
VSLALADLSVAVAVMPFVSVTDLIGGKWIFGHFFCNVFIAMDVMCCTASIMTLCVISIDR
YLGITRPLTYPVRQNGKCMAKMILSVWLLSASITLPPLFGWAQNVNDDKVCLISQDFGYT
IYSTAVAFYIPMSVMLFMYYQIYKAARKSAAKHKFPGFPRVEPDSVIALNGIVKLQKEVE
ECANLSRLLKHERKNISIFKREQKAATTLGIIVGAFTVCWLPFFLLSTARPFICGTSCSC
IPLWVERTFLWLGYANSLINPFIYAFFNRDLRTTYRSLLQCQYRNINRKLSAAGMHEALK
LAERPERPEFVLRACTRRVLLRPEKRPPVSVWVLQSPDHHNWLADKMLTTVEKKVMIHD
Target 4 Number of Residues 486
Target 4 Molecular Weight 53556
Target 4 Theoretical pI 8.97
Target 4 GO Classification
Function
peptide receptor activity, G-protein coupled
melanocortin 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 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 stimulate adenylate cyclase
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • 84-104
  • 118-138
  • 158-178
  • 202-222
  • 237-257
  • 326-346
  • 368-388
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 1857143 Link Image
Target 4 UniProtKB/Swiss-Prot ID P34969 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name 5HT7R_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 4 Gene Sequence >1440 bp 
ATGATGGACGTTAACAGCAGCGGCCGCCCGGACCTCTACGGGCACCTCCGCTCTTTCCTT
CTGCCAGAAGTGGGGCGCGGGCTGCCCGACTTGAGCCCCGACGGTGGCGCCGACCCGGTC
GCGGGCTCCTGGGCGCCGCACCTGCTGAGCGAGGTGACAGCCAGCCCGGCGCCCACCTGG
GACGCGCCCCCGGACAATGCCTCCGGCTGTGGGGAACAGATCAACTACGGCAGAGTCGAG
AAAGTTGTGATCGGCTCCATCCTGACGCTCATCACGCTGCTGACGATCGCGGGCAACTGC
CTGGTGGTGATCTCCGTGTGCTTCGTCAAGAAGCTCCGCCAGCCCTCCAACTACCTGATC
GTGTCCCTGGCGCTGGCCGACCTCTCGGTGGCTGTGGCGGTCATGCCCTTCGTCAGCGTC
ACCGACCTCATCGGGGGCAAGTGGATCTTTGGACACTTTTTCTGTAATGTCTTCATCGCC
ATGGACGTCATGTGCTGCACGGCCTCGATCATGACCCTGTGCGTGATCAGCATTGACAGG
TACCTTGGGATCACAAGGCCCCTCACATACCCTGTGAGGCAGAATGGGAAATGCATGGCG
AAGATGATTCTCTCCGTCTGGCTTCTCTCCGCCTCCATCACCTTACCTCCACTCTTTGGA
TGGGCTCAGAATGTAAATGATGATAAGGTGTGCTTGATCAGCCAGGACTTTGGCTATACG
ATTTACTCTACCGCAGTGGCATTTTATATCCCCATGTCCGTCATGCTTTTCATGTACTAC
CAGATTTACAAGGCTGCCAGGAAGAGTGCTGCCAAACACAAGTTTCCTGGCTTCCCTCGA
GTGGAGCCAGACAGCGTCATCGCCCTGAATGGCATAGTGAAGCTCCAGAAGGAGGTGGAA
GAGTGTGCAAACCTTTCGAGACTCCTCAAGCATGAAAGGAAAAACATCTCCATCTTTAAG
CGAGAACAGAAAGCAGCCACCACCCTGGGGATCATCGTCGGGGCCTTTACCGTGTGCTGG
CTGCCATTTTTCCTCCTCTCGACAGCCAGACCCTTCATCTGTGGCACTTCCTGCAGCTGC
ATCCCACTGTGGGTGGAGAGGACATTTCTGTGGCTAGGCTATGCAAACTCTCTCATTAAC
CCTTTTATATATGCCTTCTTCAACCGGGACCTGAGGACCACCTATCGCAGCCTGCTCCAG
TGCCAGTACCGGAATATCAACCGGAAGCTCTCAGCTGCAGGCATGCATGAAGCCCTGAAG
CTTGCTGAGAGGCCAGAGAGACCTGAGTTTGTGCTGAGGGCCTGCACAAGGAGGGTGCTG
TTGAGACCAGAAAAGAGGCCACCGGTATCTGTGTGGGTGCTACAATCTCCAGACCATCAC
AATTGGTTAGCAGACAAAATGCTGACTACTGTAGAAAAAAAGGTCATGATTCATGATTGA
Target 4 GenBank Gene ID
Target 4 GeneCard ID HTR7 Link Image
Target 4 GenAtlas ID HTR7 Link Image
Target 4 HGNC ID HGNC:5302 Link Image
Target 4 Chromosome Location 10
Target 4 Locus 10q21-q24
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Bard JA, Zgombick J, Adham N, Vaysse P, Branchek TA, Weinshank RL: Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. J Biol Chem. 1993 Nov 5;268(31):23422-6. [PubMed Link Image]
  2. Heidmann DE, Metcalf MA, Kohen R, Hamblin MW: Four 5-hydroxytryptamine7 (5-HT7) receptor isoforms in human and rat produced by alternative splicing: species differences due to altered intron-exon organization. J Neurochem. 1997 Apr;68(4):1372-81. [PubMed Link Image]
  3. Erdmann J, Nothen MM, Shimron-Abarbanell D, Rietschel M, Albus M, Borrmann M, Maier W, Franzek E, Korner J, Weigelt B, Fimmers R, Propping P: The human serotonin 7 (5-HT7) receptor gene: genomic organization and systematic mutation screening in schizophrenia and bipolar affective disorder. Mol Psychiatry. 1996 Nov;1(5):392-7. [PubMed Link Image]
Target 4 Drug References
  1. Sugimoto Y, Inoue K, Yamada J: The tricyclic antidepressant clomipramine increases plasma glucose levels of mice. J Pharmacol Sci. 2003 Sep;93(1):74-9. [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.