Agonistic effects of the opioid buprenorphine on the nociceptin/OFQ receptor

被引：77

作者：

Bloms-Funke, P ^{[1
]}

Gillen, C ^{[1
]}

Schuettler, AJ ^{[1
]}

Wnendt, S ^{[1
]}

机构：

[1] Grunenthal GmbH, D-52078 Aachen, Germany

来源：

PEPTIDES | 2000年 / 21卷 / 07期

关键词：

opioids; ORL1; nociceptin/orphanin FQ; Xenopus oocytes; potassium currents; GTP gamma S; CHO-K1; cells; analgesia;

D O I：

10.1016/S0196-9781(00)00252-7

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The nociceptin/orphanin FQ (N/OFQ) receptor (e.g. the human ortholog ORL1) has been shown to be pharmacologically distinct from classic opioid receptors. Recently, we have identified buprenorphine as a full ORL1 agonist using a reporter gene assay. For further functional analysis, buprenorphine's effects on ORL1 receptors were investigated using a K+ channel (GIRK1) assay in Xenopus oocytes and GTP gamma S assay in CHO-K1 membrane preparations. Tn both assays, buprenorphine behaved as a partial agonist compared to nociceptin itself. The N/OFQ agonism of buprenorphine might contribute to actions of buprenorphine in pain models in vivo beside its mu- or kappa-opioid receptor mediated effects. (C) 2000 Elsevier Science Inc. All rights reserved.

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页码：1141 / 1146

页数：6

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