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Titolo:
A potent and highly selective nonpeptidyl nociceptin/orphanin FQ receptor (ORL1) antagonist: J-113397
Autore:
Ozaki, S; Kawamoto, H; Itoh, Y; Miyaji, M; Iwasawa, Y; Ohta, H;
Indirizzi:
Banyu Pharmaceut Co Ltd, Merck Res Labs, Banyu Tsukuba Res Inst, Tsukuba, Ibaraki 3002611, Japan Banyu Pharmaceut Co Ltd Tsukuba Ibaraki Japan 3002611 raki 3002611, Japan
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 3, volume: 387, anno: 2000,
pagine: R17 - R18
SICI:
0014-2999(20000117)387:3<R17:APAHSN>2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
AGONIST;
Keywords:
nociceptin/orphanin FQ; ORL1 receptor; opioid;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
7
Recensione:
Indirizzi per estratti:
Indirizzo: Ozaki, S Banyu Pharmaceut Co Ltd, Merck Res Labs, Banyu Tsukuba Res Inst, 3 Okubo, Tsukuba, Ibaraki 3002611, Japan Banyu Pharmaceut Co Ltd 3 Okubo Tsukuba Ibaraki Japan 3002611 pan
Citazione:
S. Ozaki et al., "A potent and highly selective nonpeptidyl nociceptin/orphanin FQ receptor (ORL1) antagonist: J-113397", EUR J PHARM, 387(3), 2000, pp. R17-R18

Abstract

We discovered a potent nociceptin/orphanin FQ receptor (ORL1) receptor antagonist, J-113397 (1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one). J-113397 inhibited [I-125][Tyr(14)]nociceptin binding to Chinese hamster ovary (CHO) cells expressing ORL1 receptor in a dose-dependent manner (IC50; 2.3 nM), but showed 600-foldor less affinity for mu-, delta- and kappa-opioid receptors. Nociceptin/orphanin FQ-induced suppression of cyclic AMP accumulation elicited by forskolin was completely inhibited by J-113397 with an IC50 value of 26 nM. Theseresults indicate that J-113397 is a potent and selective nonpeptidyl antagonist of the ORL1 receptor. (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 08/04/20 alle ore 10:16:57