Kinetics of Respiratory Depression in Rats Induced by Buprenorphine and its Metabolite, Norbuprenorphine

摘要: The respiratory depression induced by buprenorphine and its active metabolite, norbuprenorphine (NBN), was evaluated in rats measurement of changes rate arterial pCO2 levels. After i.v. bolus administration no effects were noted over the dose range 0.008 to 3 mg/kg; contrast, after rapid NBN decreased a dose-dependent fashion within 1 mg/kg, levels also varied relation change rate. minimum observed 15 min administration. Judging depressive effect infusion, approximately 10 times more potent than parent drug. In spite similarity concentrations brain i.a. (3 mg/kg), neither nor changed compared with control Moreover, concentration lungs 4-fold higher that NBN-induced rapidly reduced naloxone beta-funaltrexamine, but ICI 174864 without effect. These results suggest may be mediated opioid mu receptors lung rather brain.