Therapeutic Targets Database
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TTD Target ID: TTDS00100

Target Information
Name5-hydroxytryptamine 1D receptor    
Type of targetSuccessful target    
Synonyms5-HT-1D    
5-HT-1D-alpha    
5-HT1D receptor    
5-hydroxytryptamine receptor 1D    
5HT1D    
Serotonin receptor    
Serotonin receptor 1D    
DiseaseMigraine
[ICD9: 346   ICD10: G43]
[1]
Obsessive-compulsive disorder
[ICD9: 300.3   ICD10: F42]
[2]
Vascular headache
[ICD9: 339, 784.0   ICD10: G43-G44, R51]
[3]
Vomiting
[ICD9: 787   ICD10: R11]
[4]
Drug(s)AlmogranApprovedMigraine[1]
EletriptanApprovedMigraine[5][6]
FrovatriptanApprovedMigraine headaches[7]
RizatriptanApprovedAcute migraine headache[8]
SumatriptanApprovedMigraine headaches[9][10][3][4][11]
ZolmitriptanApprovedMigraine[12]
Elzasonan hydrochlorideDiscontinued in Phase IISevere Mood Disorders[13]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP28221
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.    
SequenceMSPLNQSAEGLPQEASNRSLNATETSEAWDPRTLQALKISLAVVLSVITLATVLSNAFVL TTILLTRKLHTPANYLIGSLATTDLLVSILVMPISIAYTITHTWNFGQILCDIWLSSDIT CCTASILHLCVIALDRYWAITDALEYSKRRTAGHAATMIAIVWAISICISIPPLFWRQAK AQEEMSDCLVNTSQISYTIYSTCGAFYIPSVLLIILYGRIYRAARNRILNPPSLYGKRFT TAHLITGSAGSSLCSLNSSLHEGHSHSAGSPLFFNHVKIKLADSALERKRISAARERKAT KILGIILGAFIICWLPFFVVSLVLPICRDSCWIHPALFDFFTWLGYLNSLINPIIYTVFN EEFRQAFQKIVPFRKAS
Related US Patent6,277,853
6,342,498
6,346,622
6,355,674
6,509,340
6,589,953
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+/-)-nantenine[14]
(3-Chloro-phenyl)-piperazin-1-yl-methanone[15]
1,2,3,4-Tetrahydro-naphthalen-2-ylamine[16]
1- ([17]
1- (2,5-Dimethoxy-4-methyl-phenyl)-piperazine[15]
1- (2,5-Dimethoxy-phenyl)-piperazine[15]
1- (2-Butoxy-phenyl)-piperazine[18]
1- (2-Ethoxy-phenyl)-piperazine[18]
1- (2-Fluoro-phenyl)-piperazine[18]
1- (2-Isopropoxy-phenyl)-piperazine[18]
1- (2-Methoxy-phenyl)-piperazine[18]
1- (3-[19]
1- (3-Fluoro-phenyl)-piperazine[18]
1- (3-Nitro-phenyl)-piperazine[18]
1- (3-Trifluoromethyl-phenyl)-piperazine[15]
1- (4-Bromo-2,5-dimethoxy-phenyl)-piperazine[15]
1- (7-Methoxy-naphthalen-2-yl)-piperazine[20]
1-Naphthalen-1-yl-piperazine[16]
1-Naphthalen-2-yl-piperazine[16]
2- (2,5-Dimethoxy-phenyl)-1-methyl-ethylamine[21]
2- (2,6-Dimethyl-benzyl)-4,5-dihydro-1H-imidazole[22]
2- (2-Amino-propyl)-5-bromo-4-methoxy-phenol[21]
2- (2-Methoxy-phenyl)-1-methyl-ethylamine[21]
2- (3-Methoxy-phenyl)-1-methyl-ethylamine[21]
2- (4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine[21]
2- (4-Bromo-phenyl)-1-methyl-ethylamine[21]
2- (4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole[22]
2- (5-Nonyloxy-1H-indol-3-yl)-ethylamine[23]
2- (5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine[24]
2-Piperazin-1-yl-benzonitrile[18]
2-Piperazin-1-yl-phenol[15]
3-Amino-1- (2-amino-5-methoxy-phenyl)-propan-1-one[15]
5,6-dichloro-3,4-dihydroquinazolin-2-amine[25]
5-Ethyl-3- (2-pyrrolidin-1-yl-ethyl)-1H-indole[26]
5-Isopropyl-3- (2-pyrrolidin-1-yl-ethyl)-1H-indole[26]
5-amino-3- (N-methylpiperidin-4-yl)-1H-indole[27]
5-chloro-3,4-dihydroquinazolin-2-amine[25]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine[25]
8-Methoxy-2- (4-methyl-piperazin-1-yl)-quinoline[16]
8-Methoxy-2-piperazin-1-yl-quinoline[16]
8-Methoxy-quinolin-2-ylamine[16]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine[25]
AGROCLAVINE[28]
Brolamfetamine[21]
CHLOROPHENYLPIPERAZINE[18]
Etisulergine[29]
GR-127935[30]
L-741604[31]
L-747201[32]
L-760790[31]
L-775606[27]
LY-334370[27]
PHENYLPIPERAZINE[16]
QUIPAZINE[16]
SB-224289[33]
SEROTONIN[27]
WAY-466[34]
[2- (5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine[26]
AgonistAlmogran[1]
Eletriptan[5][6]
Frovatriptan[7]
Rizatriptan[8]
Sumatriptan[9][10][3][4][11]
Zolmitriptan[12]
AntagonistElzasonan hydrochloride[13]
MultitargetEletriptan[5][6]
Elzasonan hydrochloride[13]
Frovatriptan[7]
Zolmitriptan[12]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Efficacy and tolerability of subcutaneous almotriptan for the treatment of acute migraine: a randomized, double-blind, parallel-group, dose-finding study. Clin Ther. 2001 Nov;23(11):1867-75. To Reference
Ref 25-HT 1B/D receptor antagonists. Gen Pharmacol. 1997 Sep;29(3):293-303. To Reference
Ref 35-Hydroxytryptamine receptor agonists for the abortive treatment of vascular headaches block mast cell, endothelial and platelet activation within the rat dura mater after trigeminal stimulation. Brain Res. 1992 Jun 26;583(1-2):137-49. To Reference
Ref 4Novel approaches to the treatment of nausea and vomiting. Dig Dis. 1999;17(3):125-32. To Reference
Ref 5Spotlight on eletriptan in migraine. CNS Drugs. 2006;20(11):961-4. To Reference
Ref 6Eletriptan: a review of its use in the acute treatment of migraine. Drugs. 2006;66(8):1129-49. To Reference
Ref 7Frovatriptan for the acute treatment of migraine and prevention of predictable menstrual migraine. Expert Rev Neurother. 2008 May;8(5):723-36. To Reference
Ref 8An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210. To Reference
Ref 9Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32. To Reference
Ref 105-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 11Serotonin in migraine: theories, animal models and emerging therapies. Prog Drug Res. 1998;51:219-44. To Reference
Ref 12Clinical pharmacology of the serotonin receptor agonist, zolmitriptan. Expert Opin Drug Metab Toxicol. 2007 Dec;3(6):899-911. To Reference
Ref 13Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. To Reference
Ref 14Bioorg 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 15J Med Chem. 1986 May;29(5):630-4.Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents. To Reference
Ref 16J Med Chem. 1986 Nov;29(11):2375-80.5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. To Reference
Ref 17J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. To Reference
Ref 18J Med Chem. 1989 May;32(5):1052-6.Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy. To Reference
Ref 19Bioorg 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 20J Med Chem. 1997 Nov 21;40(24):3974-8.5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. To Reference
Ref 21J Med Chem. 1986 Feb;29(2):194-9.5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues. To Reference
Ref 22Bioorg Med Chem Lett. 2004 Sep 20;14(18):4697-9.2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands. To Reference
Ref 23J Med Chem. 1994 Sep 2;37(18):2828-30.5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist. To Reference
Ref 24Bioorg 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 25Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. Epub 2007 Oct 30.Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. To Reference
Ref 26Bioorg 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 27J 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 28J Med Chem. 1988 Aug;31(8):1512-9.Ergolines as selective 5-HT1 agonists. To Reference
Ref 29J Med Chem. 1985 Oct;28(10):1540-2.Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. To Reference
Ref 30Bioorg Med Chem Lett. 2005 Nov 1;15(21):4786-9.Synthesis of potent and selective serotonin 5-HT1B receptor ligands. To Reference
Ref 31J Med Chem. 1999 Feb 25;42(4):691-705.3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents. To Reference
Ref 32J Med Chem. 1997 Oct 24;40(22):3501-3.Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. To Reference
Ref 33Bioorg. Med. Chem. Lett. 7(24):3183-3188 (1997) To Reference
Ref 34J 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



 

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