The effect of anesthetics on opioid receptor

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The effects of volatile anesthetics and intravenous anesthetics on the mu-opioid receptor functions were analyzed by using oocytes expressing mu-opioid receptors-Gqi5. Volatile anesthetics inhibited the DAMGO-induced Cl- currents at clinically used concentrations. Intravenous anesthetics, ketamine inhibited, but propofol had little effects on it. Tramadol has been used as an analgesic for several decades. mu-opioid receptors are the major receptors that mediate the analgesic effects of opioids. Although mu-opioid receptors have been thought to be one of the sites of action of tramadol, there has been no report that directly proves whether the tramadol is an agonist of mu-opioid receptor or not. In this study, we examined the effects of tramadol and its main active metabolite O-Desmethyltramadol (M1), on the function of mu-opioid receptors using Xenous oocytes expressing cloned human mu-opioid receptors.