Neuropeptide Y receptor Y5 explained

Neuropeptide Y receptor type 5 is a protein that in humans is encoded by the NPY5R gene.^{[1] [2] [3]}

Selective ligands

Agonists

• Neuropeptide Y (endogenous agonist, non subtype selective)
• BWX-46 (selective NPY₅ agonist, CAS# 172997-92-1)
• Peptide YY

Antagonists

• CGP-71683 (CAS# 192322-50-2)
• FMS-586^[4]
• L-152,804 (CAS# 6508-43-6)
• Lu AA-33810^[5]
• MK-0557^[6]
• NTNCB (CAS# 486453-65-0)^[7]
• Velneperit (S-2367)

See also

• Neuropeptide Y receptor

Further reading

• Parker E, Van Heek M, Stamford A . Neuropeptide Y receptors as targets for anti-obesity drug development: perspective and current status . European Journal of Pharmacology . 440 . 2–3 . 173–87 . Apr 2002 . 12007534 . 10.1016/S0014-2999(02)01427-9 .
• Hu Y, Bloomquist BT, Cornfield LJ, DeCarr LB, Flores-Riveros JR, Friedman L, Jiang P, Lewis-Higgins L, Sadlowski Y, Schaefer J, Velazquez N, McCaleb ML . Identification of a novel hypothalamic neuropeptide Y receptor associated with feeding behavior . The Journal of Biological Chemistry . 271 . 42 . 26315–9 . Oct 1996 . 8824284 . 10.1074/jbc.271.42.26315 . free .
• Herzog H, Darby K, Ball H, Hort Y, Beck-Sickinger A, Shine J . Overlapping gene structure of the human neuropeptide Y receptor subtypes Y1 and Y5 suggests coordinate transcriptional regulation . Genomics . 41 . 3 . 315–9 . May 1997 . 9169127 . 10.1006/geno.1997.4684 .
• Nichol KA, Morey A, Couzens MH, Shine J, Herzog H, Cunningham AM . Conservation of expression of neuropeptide Y5 receptor between human and rat hypothalamus and limbic regions suggests an integral role in central neuroendocrine control . The Journal of Neuroscience . 19 . 23 . 10295–304 . Dec 1999 . 10575027 . 10.1523/JNEUROSCI.19-23-10295.1999. 6782429 . free .
• Rodriguez M, Audinot V, Dromaint S, Macia C, Lamamy V, Beauverger P, Rique H, Imbert J, Nicolas JP, Boutin JA, Galizzi JP . Molecular identification of the long isoform of the human neuropeptide Y Y5 receptor and pharmacological comparison with the short Y5 receptor isoform . The Biochemical Journal . 369 . Pt 3 . 667–73 . Feb 2003 . 12398768 . 1223119 . 10.1042/BJ20020739 .
• Berglund MM, Schober DA, Statnick MA, McDonald PH, Gehlert DR . The use of bioluminescence resonance energy transfer 2 to study neuropeptide Y receptor agonist-induced beta-arrestin 2 interaction . The Journal of Pharmacology and Experimental Therapeutics . 306 . 1 . 147–56 . Jul 2003 . 12665544 . 10.1124/jpet.103.051227 . 40163065 .
• Beauverger P, Rodriguez M, Nicolas JP, Audinot V, Lamamy V, Dromaint S, Nagel N, Macia C, Léopold O, Galizzi JP, Caignard DH, Aldana I, Monge A, Chomarat P, Boutin JA . Functional characterization of human neuropeptide Y receptor subtype five specific antagonists using a luciferase reporter gene assay . Cellular Signalling . 17 . 4 . 489–96 . Apr 2005 . 15601626 . 10.1016/j.cellsig.2004.09.006 .
• Movafagh S, Hobson JP, Spiegel S, Kleinman HK, Zukowska Z . Neuropeptide Y induces migration, proliferation, and tube formation of endothelial cells bimodally via Y1, Y2, and Y5 receptors . FASEB Journal . 20 . 11 . 1924–6 . Sep 2006 . 16891622 . 10.1096/fj.05-4770fje . free . 5566843 .
• Coletta DK, Schneider J, Stern MP, Blangero J, DeFronzo RA, Duggirala R, Jenkinson CP . Association of neuropeptide Y receptor Y5 polymorphisms with dyslipidemia in Mexican Americans . Obesity . 15 . 4 . 809–15 . Apr 2007 . 17426313 . 10.1038/oby.2007.610 . 21069742 .

External links

• Web site: Neuropeptide Y Receptors: Y₅ . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology .

Notes and References

1. Gerald C, Walker MW, Criscione L, Gustafson EL, Batzl-Hartmann C, Smith KE, Vaysse P, Durkin MM, Laz TM, Linemeyer DL, Schaffhauser AO, Whitebread S, Hofbauer KG, Taber RI, Branchek TA, Weinshank RL . A receptor subtype involved in neuropeptide-Y-induced food intake . Nature . 382 . 6587 . 168–71 . Jul 1996 . 8700207 . 10.1038/382168a0 . 1996Natur.382..168G . 4286144 .
2. Lutz CM, Richards JE, Scott KL, Sinha S, Yang-Feng TL, Frankel WN, Thompson DA . Neuropeptide Y receptor genes mapped in human and mouse: receptors with high affinity for pancreatic polypeptide are not clustered with receptors specific for neuropeptide Y and peptide YY . Genomics . 46 . 2 . 287–90 . Dec 1997 . 9417917 . 10.1006/geno.1997.5024 . free .
3. Web site: Entrez Gene: NPY5R neuropeptide Y receptor Y5.
4. Kakui N, Tanaka J, Tabata Y, Asai K, Masuda N, Miyara T, Nakatani Y, Ohsawa F, Nishikawa N, Sugai M, Suzuki M, Aoki K, Kitaguchi H . Pharmacological characterization and feeding-suppressive property of FMS586 [3-(5,6,7,8-tetrahydro-9-isopropyl-carbazol-3-yl)-1-methyl-1-(2-pyridin-4-yl-ethyl)-urea hydrochloride], a novel, selective, and orally active antagonist for neuropeptide Y Y5 receptor . The Journal of Pharmacology and Experimental Therapeutics . 317 . 2 . 562–70 . May 2006 . 16436501 . 10.1124/jpet.105.099705 . 6064389 .
5. Walker MW, Wolinsky TD, Jubian V, Chandrasena G, Zhong H, Huang X, Miller S, Hegde LG, Marsteller DA, Marzabadi MR, Papp M, Overstreet DH, Gerald CP, Craig DA . The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide] exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity . The Journal of Pharmacology and Experimental Therapeutics . 328 . 3 . 900–11 . Mar 2009 . 19098165 . 10.1124/jpet.108.144634 . 20295744 .
6. MacNeil DJ . NPY Y1 and Y5 receptor selective antagonists as anti-obesity drugs . Current Topics in Medicinal Chemistry . 7 . 17 . 1721–33 . 2007 . 17979781 . 10.2174/156802607782341028 . 2020-04-16 . https://archive.today/20130112100200/http://www.bentham-direct.org/pages/content.php?CTMC/2007/00000007/00000017/0009R.SGM . 2013-01-12 . dead .
7. Islam I, Dhanoa D, Finn J, Du P, Walker MW, Salon JA, Zhang J, Gluchowski C . Discovery of potent and selective small molecule NPY Y5 receptor antagonists . Bioorganic & Medicinal Chemistry Letters . 12 . 13 . 1767–9 . Jul 2002 . 12067557 . 10.1016/S0960-894X(02)00287-1 .