Differential Effects of Buprenorphine and Pentazocine on the Regional Cerebral Metabolic Rate for Glucose in the Conscious Rat

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The effects of buprenorphine (BNP, 10-200 μg/kg, i.v.) and pentazocine (PTZ, 2.5-10 mg/kg, i.v.) on the regional cerebral metabolic rate for glucose (rCMR_<glc>) were analyzed in nine anatomically discrete areas of the conscious rat brain by the simultaneous use of [^<14>C]2-deoxyglucose, the glucose analogue that can be phosphorylated in the brain, and [^3H]3-O-methylglucose, a nonmetabolizable glucose analogue. Originally, this method was developed by Gjedde and Diemer in the rat and in humans. The rCMR_<glc> was significantly decreased by BNP (100 or 200 μg/kg) in most of the brain regions investigated, except the cerebellum. In contrast, PTZ (10 mg/kg) significantly increased rCMR_<glc> in the cerebral cortex and medulla. In the cerebral cortex and medulla, the direction of the effect on rCMR_<glc> was opposite for BNP (22% decrease at the dose of 200 μg/kg) and PTZ (22% increase at the dose of 10 mg/kg). These findings strongly suggest that the discrepancies between the marked effects of BNP (a partial μ agonist and κ antagonist) and PTZ (a μ antagonist and κ agonist) on rCMR_<glc> reflect the selectivity of agonist action at the different types of opioid receptors, μ and κ receptors, in the rat brain.
公益社団法人日本薬学会の論文
1997-09-15