Referenced in: none

Automatically associated channels: Kir2.1 , Kir3.1

Title: Agonistic effects of the opioid buprenorphine on the nociceptin/OFQ receptor.

Authors: P Bloms-Funke, C Gillen, A J Schuettler, S Wnendt

Journal, date & volume: Peptides, 2000 Jul , 21, 1141-6

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/10998549

Abstract
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 GTPgammaS assay in CHO-K1 membrane preparations. In 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.