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Titolo:
Effects of Ro 64-6198 it nociceptin/orphanin FQ-sensitive isolated tissues
Autore:
Rizzi, D; Bigoni, R; Rizzi, A; Jenck, F; Wichmann, J; Guerrini, R; Regoli, D; Calo, G;
Indirizzi:
Univ Ferrara, Dept Expt & Clin Med, Pharmacol Sect, I-44100 Ferrara, ItalyUniv Ferrara Ferrara Italy I-44100 harmacol Sect, I-44100 Ferrara, Italy Univ Ferrara, Dept Pharmaceut Sci, I-44100 Ferrara, Italy Univ Ferrara Ferrara Italy I-44100 harmaceut Sci, I-44100 Ferrara, Italy CNS Res, Roche Pharma Div, Basel, Switzerland CNS Res Basel SwitzerlandCNS Res, Roche Pharma Div, Basel, Switzerland
Titolo Testata:
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
fascicolo: 5, volume: 363, anno: 2001,
pagine: 551 - 555
SICI:
0028-1298(200105)363:5<551:EOR6IN>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
RECEPTOR ANTAGONIST; IN-VITRO; J-113397; AGONIST; POTENT; ORL1;
Keywords:
Re 64-6198; non-peptide nociceptin, orphanin FQ receptor agonist; mouse vas deferens; guinea pig ileum; rat vas deferens;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
9
Recensione:
Indirizzi per estratti:
Indirizzo: Calo, G Univ Ferrara, Dept Expt & Clin Med, Pharmacol Sect, Via Fossato diMortara17, I-44100 Ferrara, Italy Univ Ferrara Via Fossato di Mortara 17 Ferrara Italy I-44100 taly
Citazione:
D. Rizzi et al., "Effects of Ro 64-6198 it nociceptin/orphanin FQ-sensitive isolated tissues", N-S ARCH PH, 363(5), 2001, pp. 551-555

Abstract

The pharmacological profile of the non-peptide OP4 receptor (ORL1, LC132) agonist, Bo 64-6198, was investigated, in three electrically stimulated nociceptin/orphanin FQ (NC)-sensitive preparations, namely the mouse and rat vas deferens and the guinea pig ileum. Ro 64-6193 mimicked the inhibitory effect of NC in the three preparations, while showing slow kinetics of actionand a slowly reversible effect compared to the fast and immediately and completely reversible effect of the natural peptide. Ro 64-6198 displayed similar pEC(50) and E-max values as NC in the mouse and rat vas deferens whileit was 100-fold less potent but more efficacious (higher E-max) than NC inthe guinea pig ileum. In the rat vas deferens the effects of Ro 64-6198 were antagonised by [Nphe(1)]NC(1-13)NH2 and J-113397 with pK(B) values (6.30and 8.05, respectively) similar to those obtained against NC (6.20 and 7.77, respectively). Naloxone (1 muM) was inactive. In the guinea pig ileum a clear shift of the concentration response curve to Ro 64-6198 was obtained only using a cocktail of antagonists (naloxone + [Nphe(1)]NC(1-13)NH2 or naloxone + J-113397). In the mouse vas deferens the antagonists were inactiveagainst Ro 64-6198 either when tested alone or in combination. Therefore, Ro 64-6198 behaved as a selective OP4 receptor agonist only in the rat tissue. These results suggest a physiological heterogeneity in OP4 receptors across tissues and species and may explain why, when tested in vivo, Re 64-6198 mimics the potent anxiolytic effect of NC better in the rat than in the mouse.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/05/20 alle ore 15:19:48