Therapeutic Targets Database
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TTD Target ID: TTDS00099

Target Information
Name5-hydroxytryptamine 1B receptor    
Type of targetSuccessful target    
Synonyms5-HT-1B    
5-HT-1D-beta    
5-HT1B receptor    
S12    
Serotonin 1D beta receptor    
Serotonin receptor    
Serotonin receptor 1B    
DiseaseAnxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[1]
Migraine
[ICD9: 346   ICD10: G43]
[2]
Obsessive-compulsive disorder
[ICD9: 300.3   ICD10: F42]
[3]
Pulmonary hypertension
[ICD9: 416.0   ICD10: I27.0, I27.2]
[4]
Drug(s)AlmotriptanApprovedAcute migraine headache[5]
EletriptanApprovedMigraine[6][7]
FrovatriptanApprovedMigraine headaches[8]
NaratriptanApprovedMigraine headaches[9]
ZolmitriptanApprovedMigraine[10]
Fluphenazine DecanoatePhase IIPsoriasis[11]
Elzasonan hydrochlorideDiscontinued in Phase IISevere Mood Disorders[12]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP28222
PDB Structure2G1X; 4IAQ; 4IAR.    
FunctionThis 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.    
SequenceMEEPGAQCAPPPPAGSETWVPQANLSSAPSQNCSAKDYIYQDSISLPWKVLLVMLLALIT LATTLSNAFVIATVYRTRKLHTPANYLIASLAVTDLLVSILVMPISTMYTVTGRWTLGQV VCDFWLSSDITCCTASILHLCVIALDRYWAITDAVEYSAKRTPKRAAVMIALVWVFSISI SLPPFFWRQAKAEEEVSECVVNTDHILYTVYSTVGAFYFPTLLLIALYGRIYVEARSRIL KQTPNRTGKRLTRAQLITDSPGSTSSVTSINSRVPDVPSESGSPVYVNQVKVRVSDALLE KKKLMAARERKATKTLGIILGAFIVCWLPFFIISLVMPICKDACWFHLAIFDFFTWLGYL NSLINPIIYTMSNEDFKQAFHKLIRFKCTS
Related US Patent6,277,853
6,346,622
6,509,340
6,589,953
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+/-)-nantenine[13]
1- (3-[14]
1- (7-Methoxy-naphthalen-2-yl)-piperazine[15]
1-Naphthalen-2-yl-piperazine[15]
2- (5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine[16]
5-Ethyl-3- (2-pyrrolidin-1-yl-ethyl)-1H-indole[17]
5-Isopropyl-3- (2-pyrrolidin-1-yl-ethyl)-1H-indole[17]
5-amino-3- (N-methylpiperidin-4-yl)-1H-indole[18]
A-987306[19]
GR-127935[20]
L-747201[21]
L-775606[21]
LY-334370[18]
SB-224289[20]
SEROTONIN[19]
WAY-466[22]
[2- (5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine[17]
AgonistAlmotriptan[5]
CP-94,253[1]
Eletriptan[6][7]
Frovatriptan[8]
Naratriptan[9]
SB 236057-A[23]
Zolmitriptan[10]
AntagonistElzasonan hydrochloride[12]
Fluphenazine Decanoate[11]
GR55562[4]
SB 224289[4]
MultitargetEletriptan[6][7]
Elzasonan hydrochloride[12]
Fluphenazine Decanoate[11]
Frovatriptan[8]
Zolmitriptan[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Anxiogenic-like effect of serotonin(1B) receptor stimulation in the rat elevated plus-maze. Pharmacol Biochem Behav. 2002 Apr;71(4):581-7. To Reference
Ref 25-Hydroxytryptamine(1F) receptors do not participate in vasoconstriction: lack of vasoconstriction to LY344864, a selective serotonin(1F) receptor agonist in rabbit saphenous vein. J Pharmacol Exp Ther. 1999 Sep;290(3):935-9. To Reference
Ref 35-HT 1B/D receptor antagonists. Gen Pharmacol. 1997 Sep;29(3):293-303. To Reference
Ref 45-hydroxytryptamine receptors mediating contraction in human small muscular pulmonary arteries: importance of the 5-HT1B receptor. Br J Pharmacol. 1999 Oct;128(3):730-4. To Reference
Ref 5Disposition and metabolism of almotriptan in rats, dogs and monkeys. Xenobiotica. 2006 Sep;36(9):807-23. To Reference
Ref 6Spotlight on eletriptan in migraine. CNS Drugs. 2006;20(11):961-4. To Reference
Ref 7Eletriptan: a review of its use in the acute treatment of migraine. Drugs. 2006;66(8):1129-49. To Reference
Ref 8Frovatriptan for the acute treatment of migraine and prevention of predictable menstrual migraine. Expert Rev Neurother. 2008 May;8(5):723-36. To Reference
Ref 9Triptans in pregnancy. Ther Drug Monit. 2008 Feb;30(1):5-9. To Reference
Ref 10Clinical pharmacology of the serotonin receptor agonist, zolmitriptan. Expert Opin Drug Metab Toxicol. 2007 Dec;3(6):899-911. To Reference
Ref 11Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63. To Reference
Ref 12Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. To Reference
Ref 13Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. To Reference
Ref 14Bioorg Med Chem. 2007 Nov 1;15(21):6659-66. Epub 2007 Aug 15.The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine. To Reference
Ref 15J Med Chem. 1997 Nov 21;40(24):3974-8.5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. To Reference
Ref 16Bioorg Med Chem Lett. 2000 May 1;10(9):903-5.5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine. To Reference
Ref 17Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9.5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists. To Reference
Ref 18J Med Chem. 2008 Jun 26;51(12):3609-16. Epub 2008 May 29.Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide. To Reference
Ref 19J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. To Reference
Ref 20Bioorg Med Chem Lett. 2005 Nov 1;15(21):4786-9.Synthesis of potent and selective serotonin 5-HT1B receptor ligands. To Reference
Ref 21J Med Chem. 1997 Oct 24;40(22):3501-3.Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. To Reference
Ref 22J Med Chem. 2005 Jan 27;48(2):353-6.Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. To Reference
Ref 23SB-236057-A: a selective 5-HT1B receptor inverse agonist. CNS Drug Rev. 2001 Winter;7(4):433-44. To Reference



 

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