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Titolo:
Characterisation and comparison of novel ligands for the nociceptin/orphanin FQ receptor
Autore:
Hashiba, E; Harrison, C; Calo, G; Guerrini, R; Rowbotham, DJ; Smith, G; Lambert, DG;
Indirizzi:
Univ Leicester, Dept Anaesthesia & Pain Management, LRI, Leicester LE1 5WW, Leics, England Univ Leicester Leicester Leics England LE1 5WW er LE1 5WW, Leics, England 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
Titolo Testata:
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
fascicolo: 1, volume: 363, anno: 2001,
pagine: 28 - 33
SICI:
0028-1298(200101)363:1<28:CACONL>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
NEURONS IN-VITRO; OPIOID RECEPTOR; ADENYLYL-CYCLASE; ORPHANIN-FQ; PHARMACOLOGICAL CHARACTERIZATION; NALOXONE BENZOYLHYDRAZONE; PHOSPHOLIPASE-C; ORL(1) RECEPTOR; CHO CELLS; RAT;
Keywords:
nociceptin; orphanin F/Q; nociceptin receptor agonist Ro65-6570 nociceptin receptor antagonists; [Nphe(1)]NC(1-13)NH2; J-113397 and III-BTD; radioligand binding; cAMP formation;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
37
Recensione:
Indirizzi per estratti:
Indirizzo: Lambert, DG Univ Leicester, Dept Anaesthesia & Pain Management, LRI, Leicester LE1 5WW, Leics, England Univ Leicester Leicester Leics England LE1 5WW Leics, England
Citazione:
E. Hashiba et al., "Characterisation and comparison of novel ligands for the nociceptin/orphanin FQ receptor", N-S ARCH PH, 363(1), 2001, pp. 28-33

Abstract

Studies of nociceptin/orphanin FQ (NC) have been hampered by the paucity of available ligands with activity at the nociceptin receptor (NCR). In thisstudy we have compared the agonist profile of NC and a novel NCR agonist, Ro65-6570, in a series of radioligand binding studies and effects on forskolin-stimulated cAMP formation in Chinese hamster ovary (CHO) cells expressing the recombinant human NCR (CHOhNCR) In addition, we report the effects of three antagonists, [Nphe(1)]NC(1-13)NH2, J-113397 and III-BTD, on these responses. In radioligand binding studies Ro65-6570, [Nphe(1)]NC(1-13)NH2, J-113397 and III-BTD displaced [H-3]NC with similar pK(i) values (8.4-8.8). This compares with a pK(D) of 10.2 for NC in a direct saturation experiment. [Nphe(1)]NC(1-13)NH2 and J-113397 showed at least 100-fold selectivity over classical opioid receptors. Both NC and Ro65-6570 produced a concentration-dependent inhibition of cAMP formation with pEC(50) values of 9.56 +/- 0.05 and 8.68 +/- 0.04, respectively. Maximum inhibition achieved was 100%. [Nphe(1)]NC(1-13)NH2, 5-113397 and III-BTD produced a parallel rightward shift in the concentration-response curves to both NC and Ro65-6570 with pK(B) values of similar to6.5, similar to7.5 and similar to7.7, respectively. Importantly, all three antagonists were devoid of residual agonist activity. Collectively, these data indicate the value of Ro65-6570, [Nphe(1)]NC(1-13)NH2, 5-113397 and III-BTD in studies of the physiological role played by NC. However, due to the relatively poor selectivity of Ro65-6570 and III-BTDcaution should be exercised when using tissues that co-express mu -opioid receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 16/07/20 alle ore 04:47:30