[Phe1ψ(CH2-NH)Gly2]nociceptin-(1-13)-NH2 is an agonist of the nociceptin (ORL1) receptor

被引：95

作者：

Butour, JL ^{[1
]}

Moisand, C ^{[1
]}

Mollereau, C ^{[1
]}

Meunier, JC ^{[1
]}

机构：

[1] Inst Pharmacol & Biol Struct, CNRS, UPR 9062, Unite Neuropharmacol Mol, F-31077 Toulouse 4, France

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1998年 / 349卷 / 01期

关键词：

nociceptin pseudopeptide analog; nociceptin receptor; human brain; cAMP synthesis inhibition;

D O I：

10.1016/S0014-2999(98)00273-8

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

[Phe(1)psi(CH2-NH)Gly(2)]nociceptin-(1-13)-NH2, a pseudopeptide analog of nociceptin, has been shown to be a selective 'antagonist' of the nociceptin receptor in the isolated guinea pig ileum and mouse vas deferens preparations (Guerrini et al., 1998. Br. J. Pharmacol. 123, 163-165). However, in recombinant chinese hamster ovary cells expressing the human nociceptin receptor, we find that the pseudopeptide is a potent (IC50 = 7.5 nM) and fully efficacious inhibitor of forskolin-induced accumulation of cAMP, thus behaving as a pure 'agonist' rather than an antagonist of the receptor. The contrary behaviour of the pseudopeptide in smooth muscle and transformed cells may suggest that different nociceptin receptor types are being addressed in the two systems. (C) 1998 Elsevier Science B.V. All rights reserved.

引用

页码：R5 / R6

页数：2

共 8 条

[1] A SEPARATION METHOD FOR THE ASSAY OF ADENYLYLCYCLASE, INTRACELLULAR CYCLIC-AMP, AND CYCLIC-AMP PHOSPHODIESTERASE USING TRITIUM-LABELED SUBSTRATES [J].