Agonistic effects of the opioid buprenorphine on the nociceptin/OFQ receptor.
Article Details
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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
Drug Target Kind Organism Pharmacological Action Actions Buprenorphine Nociceptin receptor Protein Humans UnknownNot Available Details