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Titolo:
Orexigenic effect of the melanocortin MC4 receptor antagonist HS014 is inhibited only partially by neuropeptide YY1 receptor selective antagonists
Autore:
Kask, A; Schioth, HB; Harro, J; Wikberg, JES; Rago, L;
Indirizzi:
Tartu State Univ, Fac Med, Dept Pharmacol, EE-50090 Tartu, Estonia Tartu State Univ Tartu Estonia EE-50090 armacol, EE-50090 Tartu, Estonia Univ Uppsala, Dept Pharmaceut Pharmacol, S-75105 Uppsala, Sweden Univ Uppsala Uppsala Sweden S-75105 t Pharmacol, S-75105 Uppsala, Sweden Melacure Therapeut AB, Uppsala, Sweden Melacure Therapeut AB Uppsala Sweden cure Therapeut AB, Uppsala, Sweden Tartu State Univ, Fac Social Sci, Dept Psychol, EE-50090 Tartu, Estonia Tartu State Univ Tartu Estonia EE-50090 Psychol, EE-50090 Tartu, Estonia
Titolo Testata:
CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY
fascicolo: 2, volume: 78, anno: 2000,
pagine: 143 - 149
SICI:
0008-4212(200002)78:2<143:OEOTMM>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
AGOUTI OBESITY SYNDROME; FOOD-INTAKE; IN-VIVO; Y1 RECEPTOR; RATS; NPY; BIBP3226; NEURONS; 1229U91; PROTEIN;
Keywords:
neuropeptide Y; NPYY1 receptor antagonist; BIBO3304; BIBP3226; [D-Tyr D-27,D-36-Thr(32)]NPY(27-36); 1229U91; food intake; MC4 receptor antagonist; HS014;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
35
Recensione:
Indirizzi per estratti:
Indirizzo: Kask, A Tartu State Univ, Fac Med, Dept Pharmacol, Ulikooli 18, EE-50090 Tartu, Estonia Tartu State Univ Ulikooli 18 Tartu Estonia EE-50090 artu, Estonia
Citazione:
A. Kask et al., "Orexigenic effect of the melanocortin MC4 receptor antagonist HS014 is inhibited only partially by neuropeptide YY1 receptor selective antagonists", CAN J PHYSL, 78(2), 2000, pp. 143-149

Abstract

Neuropeptide Y (NPY) and melanocortin (MC) peptides have opposite effects on food intake: NPY-like peptides and MC receptor antagonists stimulate feeding and increase body weight, whereas melanocortins and NPY antagonists inhibit food intake. In this study we tested whether the orexigenic effect ofthe selective MC4 receptor antagonist HS014 (1 nmol) could be inhibited bythree different NPY antagonists, (R)-N-2-(diphenylacetyl)-N-[(4-hydroxy-phenyl)methyl]- D-argininamide (BIBP3226), (R)-N-[[4-(aminocarbonylaminomethyl)-phenyl]methyl]-N-2-(diphenylacetyl)-argininamide-trifluoroacetate (BIBO3304), and decapeptide [D-Tyr(27,36)D-Thr(32)]NPY27-36, after icv administration in freely feeding male rats. All three NPY receptor antagonists inhibited the orexigenic effects of HS014 partially and with markedly different potency. [D-Tyr(27,36)D-Thr(32)]NPY27-36 was active only in subconvulsive dose. The NPY Y-1 selective antagonist BIBP3226 was more effective in inhibiting the effect of HS014 than BIBO3304 despite in vitro data indicating thatBIBP3226 is about 10 times less potent than BIBO3304 at NPY Y-1 receptor. An enantiomer of BIBO3304, BIBO3457, failed to inhibit HS014-induced feeding, indicating that the effects of BIBO3304 were stereoselective. These results suggest that stimulation of food intake caused by weakening of melanocortinergic tone at the MC4 receptor is partially but not exclusively relatedto NPY Y-1 receptor activation.

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Documento generato il 04/07/20 alle ore 23:08:53