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Titolo:
[Nphe(1)]nociceptin-(1-13)NH2 selectively antagonizes nociceptin effects in the rabbit isolated ileum
Autore:
Pheng, LH; Calo, G; Guerrini, R; Regoli, D;
Indirizzi:
Univ Sherbrooke, Inst Pharmacol Sherbrooke, Sherbrooke, PQ J1H 5N4, CanadaUniv Sherbrooke Sherbrooke PQ Canada J1H 5N4 erbrooke, PQ J1H 5N4, Canada 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 Univ Ferrara, Ctr Biotechnol, I-44100 Ferrara, Italy Univ Ferrara Ferrara Italy I-44100 tr Biotechnol, I-44100 Ferrara, Italy
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 2-3, volume: 397, anno: 2000,
pagine: 383 - 388
SICI:
0014-2999(20000602)397:2-3<383:[SANEI>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
ORL1 RECEPTOR; IN-VITRO; PHARMACOLOGICAL CHARACTERIZATION; INTERNATIONAL UNION; VAS-DEFERENS; ORPHANIN-FQ; RAT-BRAIN; BINDING; CLASSIFICATION; NEUROPEPTIDE;
Keywords:
nociceptin; [Nphe(1)]nociceptin-(1-13)NH2; OP4 receptor; ileum, rabbit;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
32
Recensione:
Indirizzi per estratti:
Indirizzo: Regoli, D Univ Sherbrooke, Inst Pharmacol Sherbrooke, 3001,12E Ave Nord, Sherbrooke,PQ J1H 5N4, Canada Univ Sherbrooke 3001,12E Ave Nord Sherbrooke PQ Canada J1H 5N4 a
Citazione:
L.H. Pheng et al., "[Nphe(1)]nociceptin-(1-13)NH2 selectively antagonizes nociceptin effects in the rabbit isolated ileum", EUR J PHARM, 397(2-3), 2000, pp. 383-388

Abstract

When suspended in vitro in isolated organ baths, segments of the rabbit ileum show a fairly strong and stable spontaneous activity, which derives from the continuous release of acetylcholine and the activation of muscarinic receptors, since the activity is completely eliminated by atropine. Dynorphin A (pEC(50): 8.6 +/- 0.07), neuropeptide Y and its congener human pancreatic polypeptide (pEC(50): 9.40 +/- 0.10), and nociceptin (pEC(50): 8.08 +/-0.12) dose-dependently inhibit the spontaneous activity through the activation of receptors, which are specifically antagonised respectively by naloxone (pA(2): 7.17 +/- 0.12), 2-(naphtalen-1-ylamino)-3-phenylpropionitrile (JCF 104; pA(2): 5.80 +/- 0.10), and [Nphe(1)]nociceptin-(1-13)NH2 (pA(2): 6.17 +/- 0.19). This last compound, a selective nociceptin-receptor (OP4) antagonist, inhibits the effect of nociceptin in a competitive manner, as demonstrated by Schild analysis. [Nphe(1)]nociceptin-(1-13)NH2 also antagonizes the effects of other OP4 receptor ligands such as the full agonist, nociceptin-(1-13)-NH2, and the partial agonists, [Phe(1)psi(CH2-NH)Gly(2)]nociceptin-(1-13)-NH2 (intrinsic activity (alpha(E)) = 0.5) and Ac-RYYWK-NH2 (alpha(E) = 0.5), with pA(2) values ranged from 5.8 to 6.2. These results indicate that the functional site mediating the inhibitory effect of nociceptin in the rabbit ileum, is pharmacologically identical to the OP4 sites of other species (mouse, rat, guinea pig, man), since the potencies (pA(2) values) of the pure and competitive antagonist [Nphe(1)]nociceptin-(1-13)NH2 is very similar to the values obtained in the other species. Moreover, the rabbit ileum is one of the few isolated organs that allow classifying compounds, which interact with OP4 receptors as full agonists, partial agonists, or pure antagonists. (C) 2000 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 07/04/20 alle ore 02:55:57