TTD Target ID: TTDS00099

Target Information
Name	5-hydroxytryptamine 1B receptor
Type of target	Successful target
Synonyms	5-HT-1B
	5-HT-1D-beta
	5-HT1B receptor
	S12
	Serotonin 1D beta receptor
	Serotonin receptor
	Serotonin receptor 1B
Disease	Anxiety disorder, unspecified    [1]
	Migraine    [2]
	Obsessive-compulsive disorder    [3]
	Pulmonary hypertension    [4]
Drug(s)	Almotriptan		Approved	Acute migraine headache	[5]
	Eletriptan		Approved	Migraine	[6][7]
	Frovatriptan		Approved	Migraine headaches	[8]
	Naratriptan		Approved	Migraine headaches	[9]
	Zolmitriptan		Approved	Migraine	[10]
	Fluphenazine Decanoate		Phase II	Psoriasis	[11]
	Elzasonan hydrochloride		Discontinued in Phase II	Severe Mood Disorders	[12]
BioChemical Class	G-protein coupled receptor (rhodopsin family)
Pathway	Neuroactive ligand-receptor interaction
UniProt ID	P28222
PDB Structure	2G1X.
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.
Sequence	MEEPGAQCAPPPPAGSETWVPQANLSSAPSQNCSAKDYIYQDSISLPWKVLLVMLLALIT LATTLSNAFVIATVYRTRKLHTPANYLIASLAVTDLLVSILVMPISTMYTVTGRWTLGQV VCDFWLSSDITCCTASILHLCVIALDRYWAITDAVEYSAKRTPKRAAVMIALVWVFSISI SLPPFFWRQAKAEEEVSECVVNTDHILYTVYSTVGAFYFPTLLLIALYGRIYVEARSRIL KQTPNRTGKRLTRAQLITDSPGSTSSVTSINSRVPDVPSESGSPVYVNQVKVRVSDALLE KKKLMAARERKATKTLGIILGAFIVCWLPFFIISLVMPICKDACWFHLAIFDFFTWLGYL NSLINPIIYTMSNEDFKQAFHKLIRFKCTS
Related US Patent	6,277,853
	6,346,622
	6,509,340
	6,589,953
Target Validation	Click 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]
Agonist	Almotriptan		[5]
	CP-94,253		[1]
	Eletriptan		[6][7]
	Frovatriptan		[8]
	Naratriptan		[9]
	SB 236057-A		[23]
	Zolmitriptan		[10]
Antagonist	Elzasonan hydrochloride		[12]
	Fluphenazine Decanoate		[11]
	GR55562		[4]
	SB 224289		[4]
Multitarget	Eletriptan		[6][7]
	Elzasonan hydrochloride		[12]
	Fluphenazine Decanoate		[11]
	Frovatriptan		[8]
	Zolmitriptan		[10]
Cross References	3D Structure Related Literature On-Line Medical Dictionary
Ref 1	Anxiogenic-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 2	5-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 3	5-HT 1B/D receptor antagonists. Gen Pharmacol. 1997 Sep;29(3):293-303. To Reference
Ref 4	5-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 5	Disposition and metabolism of almotriptan in rats, dogs and monkeys. Xenobiotica. 2006 Sep;36(9):807-23. To Reference
Ref 6	Spotlight on eletriptan in migraine. CNS Drugs. 2006;20(11):961-4. To Reference
Ref 7	Eletriptan: a review of its use in the acute treatment of migraine. Drugs. 2006;66(8):1129-49. To Reference
Ref 8	Frovatriptan for the acute treatment of migraine and prevention of predictable menstrual migraine. Expert Rev Neurother. 2008 May;8(5):723-36. To Reference
Ref 9	Triptans in pregnancy. Ther Drug Monit. 2008 Feb;30(1):5-9. To Reference
Ref 10	Clinical pharmacology of the serotonin receptor agonist, zolmitriptan. Expert Opin Drug Metab Toxicol. 2007 Dec;3(6):899-911. To Reference
Ref 11	Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63. To Reference
Ref 12	Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. To Reference
Ref 13	Bioorg 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 14	Bioorg 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 15	J Med Chem. 1997 Nov 21;40(24):3974-8.5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. To Reference
Ref 16	Bioorg 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 17	Bioorg 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 18	J 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 19	J 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 20	Bioorg Med Chem Lett. 2005 Nov 1;15(21):4786-9.Synthesis of potent and selective serotonin 5-HT1B receptor ligands. To Reference
Ref 21	J Med Chem. 1997 Oct 24;40(22):3501-3.Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. To Reference
Ref 22	J 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 23	SB-236057-A: a selective 5-HT1B receptor inverse agonist. CNS Drug Rev. 2001 Winter;7(4):433-44. To Reference

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.

Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore

All rights reserved.