PMID- 9802437 OWN - NLM STAT- MEDLINE DCOM- 19990119 LR - 20190831 IS - 0167-0115 (Print) IS - 0167-0115 (Linking) VI - 75-76 DP - 1998 Sep 25 TI - NPY-induced feeding involves the action of a Y1-like receptor in rodents. PG - 409-15 AB - We have reported that the potent peptidic Y1 antagonist, 1229U91, significantly suppressed NPY-induced and spontaneous feeding [32,33]. However, information on the precise selectivity of 1229U91 for NPY receptors is lacking. The Y5 receptor has been considered a key receptor for feeding regulation. In the present study we showed that 1229U91 has high affinities for the human and rat Y1 receptors (Ki = 0.041 nM and 0.16 nM, respectively) and also a high affinity for the human Y4 receptor (Ki = 0.33 nM), whereas it shows moderate affinities for the human Y2, Y5 and rat Y5 receptors (K values of 20-170 nM). Moreover, 1229U91 potently inhibits NPY-induced [Ca2+]i increases in cells expressing human Y1 receptors. In contrast, 1229U91 is an agonist at other NPY receptors like the Y2, Y4 and Y5 receptors. Intracerebroventricular (i.c.v.)-injected 1229U91 (30 microg/head) significantly suppressed human NPY-induced feeding in SD rats, while 1229U91 only moderately inhibited bovine pancreatic polypeptide (bPP; an in vivo Y5 agonist)-induced feeding. These results indicate that the food intake evoked by NPY might be mediated by the Y1 receptor, rather than the Y5 receptor. Thus, the Y1 receptor or possibly a novel Y1-like receptor sensitive to 1229U91 may play a key role in the regulation of NPY-induced feeding. FAU - Kanatani, A AU - Kanatani A AD - Tsukuba Research Institute, Banyu Pharmaceutical Co. Ltd., Okubo, Japan. kantniak@banyu.co.jp FAU - Ito, J AU - Ito J FAU - Ishihara, A AU - Ishihara A FAU - Iwaasa, H AU - Iwaasa H FAU - Fukuroda, T AU - Fukuroda T FAU - Fukami, T AU - Fukami T FAU - MacNeil, D J AU - MacNeil DJ FAU - Van der Ploeg, L H AU - Van der Ploeg LH FAU - Ihara, M AU - Ihara M LA - eng PT - Journal Article PL - Netherlands TA - Regul Pept JT - Regulatory peptides JID - 8100479 RN - 0 (1229U91) RN - 0 (Neuropeptide Y) RN - 0 (Peptides, Cyclic) RN - 0 (Receptors, Neuropeptide Y) RN - 0 (neuropeptide Y-Y1 receptor) RN - 0 (neuropeptide Y5 receptor) RN - 59763-91-6 (Pancreatic Polypeptide) SB - IM MH - Animals MH - CHO Cells MH - COS Cells MH - Cattle MH - Cell Line MH - Cricetinae MH - Eating/*drug effects/*physiology MH - Humans MH - Injections, Intraventricular MH - Kinetics MH - Male MH - Neuropeptide Y/*pharmacology/physiology MH - Pancreatic Polypeptide/pharmacology MH - Peptides, Cyclic/administration & dosage/pharmacology MH - Rats MH - Rats, Sprague-Dawley MH - Receptors, Neuropeptide Y/agonists/antagonists & inhibitors/*drug effects/*physiology EDAT- 1998/11/05 00:00 MHDA- 1998/11/05 00:01 CRDT- 1998/11/05 00:00 PHST- 1998/11/05 00:00 [pubmed] PHST- 1998/11/05 00:01 [medline] PHST- 1998/11/05 00:00 [entrez] AID - S0167-0115(98)00096-2 [pii] AID - 10.1016/s0167-0115(98)00096-2 [doi] PST - ppublish SO - Regul Pept. 1998 Sep 25;75-76:409-15. doi: 10.1016/s0167-0115(98)00096-2.