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

Article Details

Citation
Copy to clipboard

Bloms-Funke P, Gillen C, Schuettler AJ, Wnendt S

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

Peptides. 2000 Jul;21(7):1141-6.

PubMed ID
10998549 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
BuprenorphineNociceptin receptorProteinHumans
Unknown
Not AvailableDetails