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

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 ef...

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Veröffentlicht in:Peptides (New York, N.Y. : 1980) N.Y. : 1980), 2000-07, Vol.21 (7), p.1141-1146
Hauptverfasser: Bloms–Funke, Petra, Gillen, Clemens, Schuettler, Achim J, Wnendt, Stephan
Format: Artikel
Sprache:eng
Schlagworte:
Analgesia
Analgesics, Opioid - pharmacology
Animals
Barium Compounds - pharmacology
Buprenorphine - pharmacology
Chlorides - pharmacology
CHO Cells
CHO-K1 cells
Cricetinae
Dose-Response Relationship, Drug
Genes, Reporter
GTPγS
Guanosine 5'-O-(3-Thiotriphosphate) - metabolism
Naloxone - pharmacology
Narcotic Antagonists - pharmacology
Nociceptin/Orphanin FQ
Oocytes - drug effects
Opioids
ORL1
Patch-Clamp Techniques
Potassium Channels - drug effects
Potassium currents
Protein Binding
Receptors, Opioid - agonists
Receptors, Opioid - metabolism
Xenopus
Xenopus oocytes
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Zusammenfassung: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 GTPγS 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 μ- or κ-opioid receptor mediated effects.
ISSN:0196-9781
1873-5169
DOI:10.1016/S0196-9781(00)00252-7