T. Suzuki et al., DIFFERENTIAL-EFFECTS OF BUPRENORPHINE AND PENTAZOCINE ON THE REGIONALCEREBRAL METABOLIC-RATE FOR GLUCOSE IN THE CONSCIOUS RAT, Biological & pharmaceutical bulletin, 20(9), 1997, pp. 997-1001
The effects of buprenorphine (BNP, 10-200 mu g/kg, i.v.) and pentazoci
ne (PTZ, 2.5-10 mg/kg, i.v.) on the regional cerebral metabolic rate f
or glucose (rCMR(glc)) mere analyzed in nine anatomically discrete are
as of the conscious rat brain by the simultaneous use of [C-14]2-deoxy
glucose, the glucose analogue that can be phosphorylated in the brain,
and [H-3]3-O-methylglucose, a nonmetabolizable glucose analogue. Orig
inally, this method was developed by Gjedde and Diemer in the rat and
in humans. The rCMR(glc) was significantly decreased by BNP (100 or 20
0 mu g/kg) in most of the brain regions investigated, except the cereb
ellum. In contrast, PTZ (10 mg/kg) significantly increased rCMR(glc) i
n the cerebral cortex and medulla. In the cerebral cortex and medulla,
the direction of the effect on rCMR(glc) was opposite for BNP (22% de
crease at the dose of 200 mu g/kg) and PTZ (22% increase at the dose o
f LO mg/kg). These findings strongly suggest that the discrepancies be
tween the marked effects of BNP (a partial mu agonist and kappa antago
nist) and PTZ (a mu antagonist and kappa agonist) on rCMR(glc) reflect
the selectivity of agonist action at the different types of opioid re
ceptors, mu and kappa receptors, in the rat brain.