Sevoflurane inhibits the μ opioid receptor-mediated signaling expressed in Xenopus oocytes.
Sevoflurane inhibits the μ opioid receptor-mediated signaling expressed in Xenopus oocytes.
复制标题
七氟烷抑制非洲爪蟾卵母细胞中表达的μ阿片受体介导的信号传导。
作者：
Minami K;Yokoyama T;Sudo Y;Ogata J;Seo M;Uezono Y
七氟醚被广泛用于麻醉，临床上常与阿片类药物联合使用。然而，七氟醚对微阿片受体功能的影响仍不清楚。在本研究中，通过使用表达与嵌合G-α蛋白Gq5(uOR-Gq5)融合的uOR的异种卵母细胞来分析七氟醚对uOR功能的影响。七氟醚本身不能在卵母细胞上诱发任何表达µOR-GQI5的电流，而在临床使用的浓度下，七氟醚可抑制[D-Ala2，N-Me-Phe4，Gly5-ol]-脑啡肽(DAMGO)诱发的氯电流。七氟醚不影响AlF4-诱导的氯电流，而AlF4-可直接激活G蛋白。在蛋白激酶C(PKC)抑制剂GF109203X处理的卵母细胞上，未观察到七氟醚对DAMGO诱发电流的抑制作用。这些结果表明，七氟醚会抑制uOR功能。此外，七氟醚抑制作用的机制可能是由PKC介导的。
Sevoflurane is widely used for anesthesia, and is commonly used together with opioids in clinical practice. However, the effects of sevoflurane on µ-opioid receptor (µOR) functions is still unclear. In this study, the effects of sevoflurane on µOR functions were analyzed by usingXenopusoocytes expressing a µOR fused to chimeric Gα protein Gqi5(µOR-Gqi5). Sevoflurane by itself did not elicit any currents in oocytes expressing µOR-Gqi5, whereas sevoflurane inhibited the [D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin (DAMGO)-induced Cl–currents at clinically used concentrations. Sevoflurane did not affect the Cl–currents induced by AlF4–, which directly led to activation of G proteins. The inhibitory effects of sevoflurane on the DAMGO-induced currents were not observed in oocytes pretreated with the protein kinase C (PKC) inhibitor GF109203X. These findings suggest that sevoflurane would inhibit µOR function. Further, the mechanism of inhibition by sevoflurane would be mediated by PKC.