Target Validation Information
Target ID T10670
Target Name Neuropeptide Y receptor type 2
Target Type
Research
Drug Potency against Target PYY(22-36) Drug Info Ki = 3 nM [528484]
AcPYY(26-36) Drug Info Ki = 670 nM [528484]
H-[Trp-Arg-Nva-Arg-Tyr]2-NH2 Drug Info Ki = 1050 nM [528136]
Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info Ki = 390 nM [528136]
Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2 Drug Info Ki = 890 nM [528136]
AcPYY(25-36) Drug Info Ki = 30 nM [528484]
AcNPY(25-36) Drug Info Ki = 75 nM [528484]
PYY(25-36) Drug Info Ki = 270 nM [528484]
Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info Ki = 310 nM [528136]
Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info Ki = 360 nM [528136]
LRHYLNLLTRQRY-NH2 Drug Info Ki = 5 nM [528667]
AcPYY(22-36) Drug Info Ki = 9 nM [528484]
H-[Trp-Arg-Nva-Arg-Tyr]3-NH2 Drug Info Ki = 50 nM [528136]
PYY3-36 Drug Info IC50 = 1.3 nM [552305]
Action against Disease Model PYY3-36 Pharmacological 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 hypothalamicand brainstem, and brain regions involved in reward processing [552896] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations The 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. [528484]
References
Ref 528484Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists.
Ref 528484Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists.
Ref 528136J 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.
Ref 528136J 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.
Ref 528136J 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.
Ref 552896The role of peptide YY in appetite regulation and obesity. J Physiol. 2009 Jan 15;587(1):19-25. doi: 10.1113/jphysiol.2008.164269. Epub 2008 Dec 8.
Ref 528484Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists.
Ref 528484Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists.
Ref 528484Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists.
Ref 528136J 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.
Ref 528136J 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.
Ref 528667Bioorg 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.
Ref 528484Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists.
Ref 528136J 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.
Ref 552305Gut hormone PYY(3-36) physiologically inhibits food intake. Nature. 2002 Aug 8;418(6898):650-4.

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