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Titolo:
Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat
Autore:
Adan, RAH; Szklarczyk, AW; Oosterom, J; Brakkee, JH; Nijenhuis, WAJ; Schaaper, WMM; Meloen, RH; Gispen, WH;
Indirizzi:
Univ Utrecht, Rudolf Magnus Inst Neurosci, Dept Med Pharmacol, NL-3508 TA Utrecht, Netherlands Univ Utrecht Utrecht Netherlands NL-3508 TA 3508 TA Utrecht, Netherlands DLO, ID, Dept Mol Recognit, NL-8200 AB Lelystad, Netherlands DLO Lelystad Netherlands NL-8200 AB it, NL-8200 AB Lelystad, Netherlands
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 3, volume: 378, anno: 1999,
pagine: 249 - 258
SICI:
0014-2999(19990813)378:3<249:COMRLO>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
MELANOCYTE-STIMULATING-HORMONE; ALPHA-MELANOTROPIN; AGOUTI; ANTAGONIST; IDENTIFICATION; EXPRESSION; PEPTIDES; PROTEIN; HYPOTHALAMUS; INDUCTION;
Keywords:
melanocortin receptor; ligand-receptor interaction; grooming behavior; MSH (melanocyte-stimulating hormone); ACTH (adrenocorticotrope hormone); stress;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
33
Recensione:
Indirizzi per estratti:
Indirizzo: Adan, RAH Univ Utrecht, Fac Med, Rudolf Magnus Inst Neurosci, Dept Med Pharmacol, Univ Weg 100, NL-3584 CG Utrecht, Netherlands Univ Utrecht Univ Weg100 Utrecht Netherlands NL-3584 CG rlands
Citazione:
R.A.H. Adan et al., "Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat", EUR J PHARM, 378(3), 1999, pp. 249-258

Abstract

Since the melanocortin MC3 and melanocortin MC4 receptors are the main melanocortin receptor subtypes expressed in rat brain, we characterized the activity and affinity of nine melanocortin receptor ligands using these receptors in vitro, as well as their activity in a well-defined melanocortin-induced behavior in the rat: grooming behavior. We report here that [D-Tyr(4)]melanotan-II and RMI-2001 (Ac-cyclo-[Cys(4), Gly(5), D-Phe(7), Cys(10)]alpha-MSH-NH2) have significantly higher affinity and potency on the rat melanocortin MC4 receptor as compared to the rat melanocortin MC3 receptor. Nle-gamma-MSH (melanocyte-stimulating hormone) was the only ligand with higher affinity and potency on the rat melanocortin MC3 receptor. The potency orderof melanocortin MC4 receptor agonists, but not that of melanocortin MC3 receptor agonists, fitted with the potency of these ligands to stimulate grooming behavior, when administered intracerebroventricularly. SHU9119 (Ac-cyclo-[Nle(4), Asp(5), D-Nal(2)(7), Lys(10)]alpha-MSH-(4-10)-NH2) and RMI-2005(Ac-cyclo-[Cys(4), Gly(5), D-Nal(2)(7), Nal(2)(9), Cys(10)]alpha-MSH-(4-10)-NH2) were able to inhibit alpha-MSH-induced melanocortin receptor activity in vitro, as well as alpha-MSH-induced grooming behavior. Melanotan-II, [Nle(4)-D-Phe(7)]alpha-MSH and RMI-2001 were also effective in inducing grooming behavior when administered intravenously. In the absence of purely selective melanocortin MC3/4 receptor ligands, we demonstrated that careful comparison of ligand potencies in vitro with ligand potencies in vivo, could identify which melanocortin receptor subtype mediated alpha-MSH-induced grooming behavior. Furthermore, blockade of novelty-induced grooming behavior by SHU9119 demonstrated that this physiological stress response is mediatedvia activation of the melanocortin system. (C) 1999 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/03/20 alle ore 12:18:49