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.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Analgesics, Opioid / pharmacology
-
Animals
-
Barium Compounds / pharmacology
-
Buprenorphine / pharmacology*
-
CHO Cells
-
Chlorides / pharmacology
-
Cricetinae
-
Dose-Response Relationship, Drug
-
Genes, Reporter
-
Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
-
Naloxone / pharmacology
-
Narcotic Antagonists / pharmacology
-
Nociceptin Receptor
-
Oocytes / drug effects
-
Patch-Clamp Techniques
-
Potassium Channels / drug effects
-
Protein Binding
-
Receptors, Opioid / agonists*
-
Receptors, Opioid / metabolism
-
Xenopus
Substances
-
Analgesics, Opioid
-
Barium Compounds
-
Chlorides
-
Narcotic Antagonists
-
Potassium Channels
-
Receptors, Opioid
-
barium chloride
-
Naloxone
-
Guanosine 5'-O-(3-Thiotriphosphate)
-
Buprenorphine
-
Nociceptin Receptor