Agonistic effects of the opioid buprenorphine on the nociceptin/OFQ receptor.
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.
Bloms-Funke
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Grünenthal GmbH, Zieglerstr. 6, D-52078, Aachen, Germany.
Gillen
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C
Schuettler
A J
AJ
Wnendt
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S
D000701:Analgesics, Opioid / Q000494:pharmacology; D000818:Animals; D017609:Barium Compounds / Q000494:pharmacology; D002047:Buprenorphine / Q000494:pharmacology*; D016466:CHO Cells; D002712:Chlorides / Q000494:pharmacology; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D017930:Genes, Reporter; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D009270:Naloxone / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000494:pharmacology; D009865:Oocytes / Q000187:drug effects; D018408:Patch-Clamp Techniques; D015221:Potassium Channels / Q000187:drug effects; D011485:Protein Binding; D011957:Receptors, Opioid / Q000819:agonists* / Q000378:metabolism; D014981:Xenopus; D000094942:Nociceptin Receptor
D000701:Analgesics, Opioid; D017609:Barium Compounds; D002712:Chlorides; D009292:Narcotic Antagonists; D015221:Potassium Channels; D011957:Receptors, Opioid; C024986:barium chloride; D009270:Naloxone; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D002047:Buprenorphine; D000094942:Nociceptin Receptor