A potent and highly selective nonpeptidyl nociceptin/orphanin FQ receptor (ORL1) antagonist: J-113397.
Eur J Pharmacol
; 387(3): R17-8, 2000 Jan 17.
Article
en En
| MEDLINE
| ID: mdl-10650183
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 [125I][Tyr(14)]nociceptin binding to Chinese hamster ovary (CHO) cells expressing ORL1 receptor in a dose-dependent manner (IC(50); 2. 3 nM), but showed 600-fold or 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 IC(50) value of 26 nM. These results indicate that J-113397 is a potent and selective nonpeptidyl antagonist of the ORL1 receptor.
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Colección:
01-internacional
Asunto principal:
Piperidinas
/
Bencimidazoles
/
Antagonistas de Narcóticos
Límite:
Animals
Idioma:
En
Revista:
Eur J Pharmacol
Año:
2000
Tipo del documento:
Article
País de afiliación:
Japón