Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00089

Target Information
NameNeuropeptide Y receptor type 5    
Type of targetClinical trial target    
SynonymsNPY-Y5 receptor    
NPY5-R    
NPYY5    
Neuropeptide Y (NPY) Y(5) receptor    
Neuropeptide Y receptor Y5    
Y5 receptor    
DiseaseEpilepsy
[ICD9: 345   ICD10: G40]
[1]
Obesity
[ICD9: 278   ICD10: E66]
[2][3][4][5]
Opioid dependence
[ICD9: 304.0   ICD10: F11.2]
[6]
Temporal lobe epilepsy
[ICD9: 345   ICD10: G40]
[7]
Drug(s)CGP71683APhase IIIObesity[2][3][5]
VelneperitPhase IIObesity[8]
Axovan-3Phase IEating disorder Obesity[9]
S-234462Phase IObesity[8]
FR-79620PreclinicalEating disorder, Obesity, Diabetes[10]
GW-594884APreclinicalObesity[10]
NPY antagonistPreclinicalObesity[10]
NPY5RA-972PreclinicalObesity[10]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDQ15761
PDB Structure2HE6.    
FunctionReceptor for neuropeptide y and peptide yy. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity. Seems to be associated with food intake. Could be involved in feeding disorders.    
SequenceMDLELDEYYNKTLATENNTAATRNSDFPVWDDYKSSVDDLQYFLIGLYTFVSLLGFMGNL LILMALMKKRNQKTTVNFLIGNLAFSDILVVLFCSPFTLTSVLLDQWMFGKVMCHIMPFL QCVSVLVSTLILISIAIVRYHMIKHPISNNLTANHGYFLIATVWTLGFAICSPLPVFHSL VELQETFGSALLSSRYLCVESWPSDSYRIAFTISLLLVQYILPLVCLTVSHTSVCRSISC GLSNKENRLEENEMINLTLHPSKKSGPQVKLSGSHKWSYSFIKKHRRRYSKKTACVLPAP ERPSQENHSRILPENFGSVRSQLSSSSKFIPGVPTCFEIKPEENSDVHELRVKRSVTRIK KRSRSVFYRLTILILVFAVSWMPLHLFHVVTDFNDNLISNRHFKLVYCICHLLGMMSCCL NPILYGFLNNGIKADLVSLIHCLHM
Related US Patent6,313,298
6,399,631
6,444,687
6,495,559
6,569,856
6,632,828
6,638,942
6,667,319
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor2,4,4-triphenylimidazoline[11]
AR-129330[12]
AR-129330[13]
ATC-0175[12]
CGP-71683A[14]
FR-226928[15]
FR-230481[15]
FR-233118[15]
FR-73966[15]
PYY (3-36)[16]
AgonistBis (31/31')[[Cys[17]
AntagonistAxovan-3[9]
CGP71683A[2][3][5]
FR-79620[10]
GW-594884A[10]
NPY antagonist[10]
NPY-5 receptor antagonist[9]
NPY5RA-972[10]
S-19528[9]
S-234462[8]
S-25585[9]
Velneperit[8]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Anticonvulsant action of neuropeptide Y. Neuropeptide Y may act as an endogenous anticonvulsant through Y5 receptors suggesting a new target for antiepileptic drugs. Nat Med. 1997 Jul;3(7):728-9. To Reference
Ref 2Neuropeptide Y-induced enhancement of the evoked release of newly synthesized dopamine in rat striatum: mediation by Y2 receptors. Neuropharmacology. 2007 May;52(6):1396-402. Epub 2007 Feb 20. To Reference
Ref 3Neuropeptide Y induced modulation of dopamine synthesis in the striatum. Regul Pept. 2005 Jul 15;129(1-3):73-8. To Reference
Ref 4Neuropeptide Y receptors as targets for anti-obesity drug development: perspective and current status. Eur J Pharmacol. 2002 Apr 12;440(2-3):173-87. To Reference
Ref 5Neuropeptide Y Y(5) receptor antagonist CGP71683A: the effects on food intake and anxiety-related behavior in the rat. Eur J Pharmacol. 2001 Mar 2;414(2-3):215-24. To Reference
Ref 6Neuropeptide Y attenuates naloxone-precipitated morphine withdrawal via Y5-like receptors. J Pharmacol Exp Ther. 1998 Feb;284(2):633-6. To Reference
Ref 7Neuropeptide Y Y5 receptors suppress in vitro spontaneous epileptiform bursting in the rat hippocampus. Neuroreport. 2004 Feb 9;15(2):339-43. To Reference
Ref 82011 Pipeline of Shionogi. To Reference
Ref 9Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36. To Reference
Ref 10Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. To Reference
Ref 11Bioorg Med Chem Lett. 2009 Mar 15;19(6):1670-4. Epub 2009 Feb 4.Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists. To Reference
Ref 12Bioorg Med Chem Lett. 2005 Sep 1;15(17):3853-6.Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1. To Reference
Ref 13Bioorg Med Chem Lett. 2005 May 16;15(10):2565-9.Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1. To Reference
Ref 14Bioorg Med Chem Lett. 2004 Feb 9;14(3):597-9.Synthesis of new thiophene and benzo[b]thiophene hydrazide derivatives as human NPY Y(5) antagonists. To Reference
Ref 15Bioorg Med Chem Lett. 2002 Mar 11;12(5):799-802.Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 3: 7-methoxy-1-hydroxy-1-substituted tetraline derivatives. To Reference
Ref 16Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists. To Reference
Ref 17Bis(31/31')[[Cys(31), Nva(34)]NPY(27-36)-NH(2)]: a neuropeptide Y (NPY) Y(5) receptor selective agonist with a latent stimulatory effect on food intake in rats. Peptides. 2002 Aug;23(8):1485-90. To Reference



 

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