GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists

European Journal of Pharmacology

Volumn 349, Issue 1, 1998, Pages 97-105

  Parker, Eric M ^a   Babij, Carol K ^a   Balasubramaniam, Ambikaipakan ^b   Burrier, Robert E ^a   Guzzi, Mario ^a   Hamud, Fozia ^a   Gitali Mukhopadhyay, ^a   Rudinski, Mark S ^a   Tao, Z ^b   Tice, Melissa ^a   Xia, Ling ^a   Mullins, Deborra E ^a   Salisbury, Brian G ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b UNIVERSITY OF CINCINNATI   (United States)

Author keywords

1229U91; GR 231118; GW 1229; Neuropeptide Y; Neuropeptide Y receptor

Indexed keywords

BW 1911U90; GR 231118; NEUROPEPTIDE Y; NEUROPEPTIDE Y1 RECEPTOR; RECEPTOR SUBTYPE; T 190; T 241; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CARBOXY TERMINAL SEQUENCE; DRUG ANTAGONISM; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; RECEPTOR BLOCKING;

AMINO ACID SEQUENCE; ANIMALS; CHO CELLS; COS CELLS; CRICETINAE; HUMANS; MICE; MOLECULAR SEQUENCE DATA; NEUROPEPTIDE Y; OLIGOPEPTIDES; PEPTIDES, CYCLIC; RADIOLIGAND ASSAY; RATS; RECEPTORS, NEUROPEPTIDE Y; TRANSFECTION;

EID: 0032524580     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(98)00171-X     Document Type: Article

References (33)

1. 32]NPY. J. Med. Chem. 39:1996;1142-1147.
2. Balasubramaniam A., Zhai W., Sheriff S., Tao Z., Chance W.T., Fischer J.E., Eden P., Taylor J. Bis(31/31′) ([Cys(31), Trp(32), Nva(34)] NPY-(31-36)): a specific NPY Y-1 receptor antagonist. J. Med. Chem. 39:1996;811-813.
3. 2 receptors. Biopolymers. 37:1995;123-142.
4. Daniels A.J., Matthews J.E., Slepetis R.J., Jansen M., Viveros O.H., Tadepalli A., Harrington W., Heyer D., Landavazo A., Leban J.J., Spaltenstein A. High-affinity neuropeptide Y receptor antagonists. Proc. Natl. Acad. Sci. USA. 92:1995;9067-9071.
5. Daniels, A.J., Heyer, D., Spaltenstein, A., 1997. Peptide antagonists of neuropeptide Y: Design, structure and pharmacological characterization. In: Grundemar, L., Bloom, S.R. (Eds.), Neuropeptide Y and Drug Development. Academic Press, San Diego, pp. 127-155.
6. DeLean A., Stadel J.M., Lefkowitz R.J. A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled β-adrenergic receptor. J. Biol. Chem. 255:1980;7108-7117.
7. Eva C., Keinanen K., Monyer H., Seeburg P., Sprengel R. Molecular cloning of a novel G protein-coupled receptor that may belong to the neuropeptide receptor family. FEBS Lett. 271:1990;81-84.
8. Feth F., Rascher W., Michel M.C. Neuropeptide Y (NPY) receptors in HEL cells: Comparison of binding and functional parameters for full and partial agonists and a non-peptide antagonist. Br. J. Pharmacol. 105:1992;71-76.
9. Gehlert D.R., Schober D.A., Beavers L., Gadski R., Hoffman J.A., Smiley D.L., Chance R.E., Lundell I., Larhammar D. Characterization of the peptide binding requirements for the cloned human pancreatic polypeptide-preferring receptor. Mol. Pharmacol. 50:1996;112-118.
10. 2) receptor and uses thereof. International patent application WO 95/21245.
11. Gerald C., Walker M.W., Criscione L., Gustafson E.L., Batzl-Hartmann C., Smith K.E., Vaysse P., Durkin M.M., Laz T.M., Linemeyer D.L., Schaffhauser A.O., Whitebread S., Hofbauer K.G., Taber R.I., Branchek T.A., Weinshank R.L. A receptor subtype involved in neuropeptide-Y-induced food intake. Nature. 382:1996;168-171.
12. 1 receptor antagonist. J. Pharmacol. Exp. Ther. 275:1995;1261-1266.
13. 5 suggests coordinate transcriptional regulation. Genomics. 41:1997;315-319.
14. Hu Y., Bloomquist B.T., Cornfield L.J., DeCarr L.B., Flores-Riveros J.R., Friedman L., Jiang P., Lewis-Higgins L., Sadlowski Y., Schaefer J., Velazquez N., McCaleb M.L. Identification of a novel hypothalamic neuropeptide Y receptor associated with feeding behavior. J. Biol. Chem. 271:1996;26315-26319.
15. 1 receptor antagonist, 1229U91: blockade of neuropeptide Y-induced and physiological food intake. Endocrinology. 137:1996;3177-3182.
16. Kenakin, T., 1993. Pharmacologic analysis of drug-receptor interaction, 2nd edn. Raven, New York, pp. 278-322.
17. Kozak M. At least six nucleotides preceding the AUG initiator codon enhance translation in mammalian cells. J. Mol. Biol. 196:1987;947-950.
18. 1 type. J. Biol. Chem. 267:1992;10935-10938.
19. 1-type receptor. J. Med. Chem. 38:1995;1150-1157.
20. Lew M.J., Murphy R., Angus J.A. Synthesis and characterization of a selective peptide antagonist of neuropeptide Y vascular postsynaptic receptors. Br. J. Pharmacol. 117:1996;1768-1772.
21. Lundell I., Blomqvist A.G., Berglund M.M., Schober D.A., Johnson D., Statnick M.A., Gadski R.A., Gehlert D.R., Larhammar D. Cloning of a human receptor of the NPY receptor family with high affinity for pancreatic polypeptide and peptide YY. J. Biol. Chem. 270:1995;29123-29128.
22. 1 receptor mediated vascular control. In: Grundemar, L., Bloom, S.R. (Eds.), Neuropeptide Y and Drug Dev., Academic Press, San Diego, pp. 41-55.
23. Michel, M.C., Beck-Sickinger, A., Cox, H., Doods, H.N., Herzog, H., Larhammar, D., Quirion, R., Schwartz, T., Westfall, T., 1998. International union of pharmacology recommendations for the nomenclature of neuropeptide Y, peptide YY and pancreatic polypeptide receptors. Pharmacol. Rev., in press.
24. 1E 5-hydroxytryptamine receptors. J. Neurochem. 67:1996;2096-2103.
25. Rose P.M., Fernandes P., Lynch J.S., Frazier S.T., Fisher S.M., Kodukula K., Kienzle B., Seethala R. Cloning and functional expression of a cDNA encoding a human type 2 neuropeptide Y receptor. J. Biol. Chem. 270:1995;22661-22664.
26. Tao, Z., Peng, G., Sheriff, S., Eden, P., Taylor, J., Chance, W.T., Balasubramaniam, A., 1997. Development of feeding and Y-1 NPY receptor antagonists. Abstracts of the Fifteenth American Peptide Symposium.
27. Turton, M.D., O'Shea, D., Bloom, S.R., 1997. Central effects of neuropeptide Y with emphasis on its role in obesity and diabetes. In: Grundemar, L., Bloom, S.R. (Eds.), Neuropeptide Y and Drug Dev., Academic Press, San Diego, pp. 15-39.
28. Wahlestedt C., Reis D.J. Neuropeptide Y-related peptides and their receptors-Are the receptor potential therapeutic drug targets? Annu. Rev. Pharmacol. Toxicol. 32:1993;309-352.
29. 2. Ann. N.Y. Acad. Sci. 611:1990;7-26.
30. 4 receptors for pancreatic polypeptide. Peptides. 18:1997;609-612.
31. Weinberg D.H., Sirinathsinghju D.J.S., Tan C.P., Shiao L.-L., Morin N., Rigby M.R., Heavens R.H., Rapoport D.R., Bayne M.L., Cascieri M.A., Strader C.D., Linemeyer D.L., MacNeil D.J. Cloning and expression of a novel neuropeptide Y receptor. J. Biol. Chem. 271:1996;16435-16438.
32. 5-like receptors. Nature Med. 3:1997;761-764.
33. Yan H., Yang J., Marasco J., Yamaguchi K., Brenner S., Collins F., Karbon W. Cloning and functional expression of cDNAs encoding human and rat pancreatic polypeptide receptors. Proc. Natl. Acad. Sci. USA. 93:1996;4661-4665.