Therapeutic Targets Database
BIDD Pharmainformatics Databases


Target Validation Information
Target NameNeuropeptide Y receptor type 2    
Type of TargetClinical trial target    
Drug Potency against TargetPYY3-36IC50 = 1.3 nM[1]
NEUROPEPTIDE-YKi = 0.081 nM[3]
PYY(3-36)Ki = 0.4 nM[4]
H-[Trp-Arg-Nva-Arg-Tyr]2-NH2Ki = 1050 nM[5]
PYY(25-36)Ki = 270 nM[4]
PYY(22-36)Ki = 3 nM[4]
AcPYY(25-36)Ki = 30 nM[4]
Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2Ki = 310 nM[5]
Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2Ki = 360 nM[5]
Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2Ki = 390 nM[5]
H-[Trp-Arg-Nva-Arg-Tyr]3-NH2Ki = 50 nM[5]
AcPYY(26-36)Ki = 670 nM[4]
AcNPY(25-36)Ki = 75 nM[4]
Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2Ki = 890 nM[5]
AcPYY(22-36)Ki = 9 nM[4]
Action against Disease ModelPYY3-36Pharmacological and genetic approaches have revealed that the Y2-receptor mediates the anorectic effects of PYY3-36 whilst mechanistic studies in rodents identified the hypothalamus, vagus and brainstem regions as potential sites of action. More recently, using functional brain imaging techniques in h uMans, PYY3-36 was found to modulate neuronal activity within hypothalamic and brainstem, and brain regions involved in reward processing[7]
The Effect of Target Knockout, Knockdown or Genetic VariationsThe Y1 receptor antagonist BIBO3304 blocked responses to the Y1 agonist at the lower doses, but only partially inhibited at the higher doses tested in Y2+/+ . In Y2+/+ receptor mice, the responses to the Y2 agonist were abolished at the lower doses and partially reduced at the highest dose tested, while those to the Y1 agonist were similar in both Y2+/+ and Y2-/-receptor mice.[8]
Ref 1Nature. 2002 Aug 8;418(6898):650-4.Gut hormone PYY(3-36) physiologically inhibits food intake. To Reference
Ref 2Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). To Reference
Ref 3J 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 4Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists. To Reference
Ref 5J Med Chem. 2006 Apr 20;49(8):2661-5.Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity. To Reference
Ref 6Bioorg Med Chem Lett. 2007 Apr 1;17(7):1916-9. Epub 2007 Jan 24.A long-acting selective neuropeptide Y2 receptor PEGylated peptide agonist reduces food intake in mice. To Reference
Ref 7J Physiol. 2009 Jan 15;587(Pt 1):19-25. Epub 2008 Dec 8.The role of peptide YY in appetite regulation and obesity. To Reference
Ref 8Br J Pharmacol. 2003 Sep;140(2):422-30. Epub 2003 Aug 26.The ability of neuropeptide Y to mediate responses in the murine cutaneous microvasculature: an analysis of the contribution of Y1 and Y2 receptors. To Reference


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