Protein kinase inhibitor potentiates opioid δ-receptor currents in Xenopus oocytes

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Abstract
IN Xenopus oocytes injected with RNA coding for the δ-opioid receptor a small chloride current was evoked by [D-Ala2,Ser5]Ieucine-enkephaline-Thr6 (DSLET), a δ2-opioid agonist. The evoked currents were rapidly reduced upon repeated challenges of DSLET. When Gilα RNA was co-injected into the oocyte, the evoked currents were increased 3.8-fold and became constant after at least three repeated challenge. In oocytes injected with RNAs coding for δ-receptor and Gilα, pretreatment with K-252a, a potent inhibitor of protein kinases, further potentiated the δ-receptor-mediated current responses, compared with those without the inhibitor. These results suggest that signalling involving the δ-opioid receptor is inactivated through in vivo phosphorylation in the Xenopus oocyte.

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