Abstract

Pentazocine, 5.6 to 56 mg/kg, caused dose-related decreases in the catecholamine content of discrete regions of the rat brain. Norepinephrine levels were lowered in all brain regions examined, whereas the depletion of dopamine was restricted to the cortex and striatum. Serotonin levels were relatively unaffected by pentazocine. Pretreatment with naloxone antagonized the pentazocine-induced depletion of brain dopamine. Naloxone also blocked the pentazocine-induced depletion of norepinephrine in the cortex and midbrain, but failed to affect the depletion of norepinephrine in the medulla and actually enhanced the depletion of hypothalamic norepinephrine. A significant depletion of medullary serotonin was observed only in rats pretreated with naloxone. These findings are consistent with the concept that pentazocine's agonistic spectrum of activity involves two components: one which is blocked by naloxone and one which is not.

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