Antagonistic effects of [Nphe1]nociceptin(1-13)NH2 on nociceptin receptor mediated inhibition of cAMP formation in Chinese hamster ovary cells stably expressing the recombinant human nociceptin receptor

被引：31

作者：

Hashimoto, Y

Caló, G

Guerrini, R

Smith, G

Lambert, DG ^{[1
]}

机构：

[1] Leicester Royal Infirm, Univ Dept Anaesthesia & Pain Management, Leicester LE1 5WW, Leics, England

[2] Univ Ferrara, Dept Expt & Clin Med, Pharmacol Sect, I-44100 Ferrara, Italy

[3] Univ Ferrara, Dept Pharmaceut Sci, I-44100 Ferrara, Italy

来源：

NEUROSCIENCE LETTERS | 2000年 / 278卷 / 1-2期

关键词：

nociceptin/orphanin FQ; antagonist; Nphe1]nociceptin(1-13)NH2; cAMP;

D O I：

10.1016/S0304-3940(99)00915-5

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

Nociceptin/orphanin FQ (NC) is the endogenous ligand for the nociceptin receptor (NCR) which is negatively coupled to adenylyl cyclase to inhibit the formation of cAMP. In this study we describe the inhibitory action of the novel NC analogue, [Nphe(1)]nociceptin(1-13)NH2 on cAMP formation in Chinese hamster ovary cells expressing the human NCR. NC, NC(1-13)NH2, the pseudopeptides [Phe(1)psi(CH2-NH)Gly(2)]NC(1-17)NH2 and [Phe(1)psi(CH2-NH)Gly(2)]NC(1-13)NH2, the hexapeptide, acetyl-Arg-Tyr-Tyr-Arg-Trp-Lys-N Hp and buprenorphine all produced a concentration dependent inhibition of forskolin stimulated cAMP formation. This inhibition was competitively reversed by [Nphe(1)] NC(1-13)NH2 with essentially identical pA(2) values (6.12-6.48). [Nphe(1)]NC(1-l3)NH2 showed per se a negligible residual agonist activity (alpha < 0.15). (C) 2000 Elsevier Science Ireland Ltd. All rights reserved.

引用

页码：109 / 112

页数：4

共 27 条

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