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Vol. 281, Issue 1, 428-433, 1997
Department of Pharmacy (M.O., H.K., T.I.) and
Department of
Anesthesiology (K.N.),
University of Tokyo Hospital, Faculty of
Medicine, University of Tokyo (Y.S.), Tokyo, Japan, and Faculty of
Pharmaceutical Sciences, Kyusyu University, Fukuoka, Japan
The respiratory depression induced by buprenorphine and its active
metabolite, norbuprenorphine (NBN), was evaluated in rats by
measurement of changes in respiratory rate and arterial
pCO2 levels. After i.v. bolus administration of
buprenorphine no effects were noted over the dose range 0.008 to 3 mg/kg; by contrast, the respiratory rate after rapid i.v.
administration of NBN decreased in a dose-dependent fashion within the
dose range of 1 to 3 mg/kg, and the arterial pCO2 levels
also varied in relation to the change in respiratory rate. The minimum
respiratory rate was observed 15 min after NBN administration. Judging
by the respiratory depressive effect after i.v. infusion, NBN was
approximately 10 times more potent than the parent drug. In spite of
the similarity of NBN concentrations in the brain after i.a. and after
i.v. administration of NBN (3 mg/kg), neither the respiratory rate nor
the arterial pCO2 levels after i.a. administration changed
compared with the control levels. Moreover, the NBN concentration in
the lungs after i.v. administration was approximately 4-fold higher
than that after i.a. administration. NBN-induced depression was rapidly reduced after i.v. administration of naloxone and 
-funaltrexamine, but ICI 174864 was without effect. These results suggest that the
respiratory depression induced by NBN may be mediated by opioid mu receptors in the lung rather than in the brain.
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