Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00157

Target Information
Name5-hydroxytryptamine 7 receptor    
Type of targetResearch target    
Synonyms5-HT-7    
5-HT-X    
5-HT7 receptor    
5HT7    
Serotonin receptor    
Serotonin receptor 7    
DiseaseMigraine
[ICD9: 346   ICD10: G43]
[1][2]
Neuropsychiatric disorders[3]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
UniProt IDP34969
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 stimulates adenylate cyclation.    
SequenceMMDVNSSGRPDLYGHLRSFLLPEVGRGLPDLSPDGGADPVAGSWAPHLLSEVTASPAPTW DAPPDNASGCGEQINYGRVEKVVIGSILTLITLLTIAGNCLVVISVCFVKKLRQPSNYLI VSLALADLSVAVAVMPFVSVTDLIGGKWIFGHFFCNVFIAMDVMCCTASIMTLCVISIDR YLGITRPLTYPVRQNGKCMAKMILSVWLLSASITLPPLFGWAQNVNDDKVCLISQDFGYT IYSTAVAFYIPMSVMLFMYYQIYKAARKSAAKHKFPGFPRVEPDSVIALNGIVKLQKEVE ECANLSRLLKHERKNISIFKREQKAATTLGIIVGAFTVCWLPFFLLSTARPFICGTSCSC IPLWVERTFLWLGYANSLINPFIYAFFNRDLRTTYRSLLQCQYRNINRKLSAAGMHEALK LAERPERPEFVLRACTRRVLLRPEKRPPVSVWVLQSPDHHNWLADKMLTTVEKKVMIHD
Related US Patent6,440,988
6,486,173
6,630,469
6,660,751
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+/-)-nantenine[4]
(2-biphenyl-3-yl-ethyl)-dimethyl-amine[5]
(R)-8-phenyl-N,N-dipropylchroman-3-amine[6]
1- (3-[7]
1-Naphthalen-1-yl-piperazine[8]
2- (1-o-tolyl-1H-pyrrol-3-yl)ethanamine[5]
2- (2'-methyl-biphenyl-3-yl)-ethylamine[5]
2- (2-Bromophenoxy)-N,N-dimethylethanamine[6]
2- (2-Bromophenylthio)-N,N-dimethylethanamine[6]
2- (Biphenyl-2-yloxy)-N,N-dimethylethanamine[6]
2- (Biphenyl-2-ylthio)-N,N-dimethylethanamine[6]
2-[1- (2-Chloro-phenyl)-1H-pyrrol-2-yl]-ethylamine[9]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[10]
5,6-dichloro-3,4-dihydroquinazolin-2-amine[11]
5-chloro-3,4-dihydroquinazolin-2-amine[11]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine[11]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine[11]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine[11]
Disulergine[8]
FALCARINDIOL[12]
IMPERATORIN[12]
L-745870[13]
MESULERGINE[14]
METHIOTHEPIN[15]
N,N-dimethyl-2- (2'-methylbiphenyl-3-yl)ethanamine[6]
SB-258719[8]
SB-258741[8]
SB-269970[8]
SB-269970[16]
SB-271046[17]
SB-656104[8]
SEROTONIN[18]
SPIPERONE[8]
UCM-5600[14]
WAY-181187[19]
WAY-208466[20]
WAY-466[21]
p-hydroxyphenethyl trans-ferulate[12]
AntagonistSB 269970-A[3]
SB 656104-A[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Is the 5-HT(7) receptor involved in the pathogenesis and prophylactic treatment of migraine? Eur J Pharmacol. 2002 Mar 29;439(1-3):1-11. To Reference
Ref 2Molecular cloning and tissue distribution of mRNA encoding porcine 5-HT7 receptor and its comparison with the structure of other species. Mol Cell Biochem. 2002 Sep;238(1-2):81-8. To Reference
Ref 35-HT7 receptors. Curr Drug Targets CNS Neurol Disord. 2004 Feb;3(1):81-90. To Reference
Ref 4Bioorg 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 5Bioorg Med Chem Lett. 2007 Jun 1;17(11):3018-22. Epub 2007 Mar 23.Novel aminoethylbiphenyls as 5-HT7 receptor ligands. To Reference
Ref 6Bioorg Med Chem. 2010 Mar 1;18(5):1958-67. Epub 2010 Jan 18.SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling. To Reference
Ref 7Bioorg 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 8J Med Chem. 2003 Jul 3;46(14):2795-812.Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). To Reference
Ref 9Bioorg Med Chem Lett. 2005 Aug 15;15(16):3753-7.Phenylpyrroles, a new chemolibrary virtual screening class of 5-HT7 receptor ligands. To Reference
Ref 10J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 11Bioorg 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 12J Nat Prod. 2006 Apr;69(4):536-41.Serotonergic activity-guided phytochemical investigation of the roots of Angelica sinensis. To Reference
Ref 13Bioorg Med Chem Lett. 2001 Jun 4;11(11):1375-7.Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands. To Reference
Ref 14J Med Chem. 2009 Apr 23;52(8):2384-92.Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity. To Reference
Ref 15Bioorg Med Chem. 2008 Mar 1;16(5):2570-8. Epub 2007 Nov 22.Novel quinazolinone derivatives as 5-HT7 receptor ligands. To Reference
Ref 16Bioorg Med Chem Lett. 2009 Aug 15;19(16):4827-31. Epub 2009 Jun 13.Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands. To Reference
Ref 17Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43. Epub 2007 Nov 17.Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. To Reference
Ref 18J Med Chem. 2008 Jul 24;51(14):4150-69. Epub 2008 Jun 28.Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. To Reference
Ref 19J Med Chem. 2007 Nov 15;50(23):5535-8. Epub 2007 Oct 19.Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist. To Reference
Ref 20Bioorg Med Chem. 2009 Jul 15;17(14):5153-63. Epub 2009 May 29.Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists. To Reference
Ref 21J 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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