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  • Title: Cyclazocine and norepinephrine uptake, metabolism, and turnover in the rat brain.
    Author: Russi GD.
    Journal: J Pharm Sci; 1985 Jan; 74(1):97-9. PubMed ID: 3981430.
    Abstract:
    The effects of cyclazocine, a narcotic agonist/antagonist, on the uptake, metabolism, and turnover of norepinephrine in rat brains were studied. Cyclazocine significantly depressed the accumulation of intracisternally administered [3H]norepinephrine and the formation of 3,4-[3H]dihydroxymandelic acid but did not alter the formation of [3H]-normetanephrine. Comparatively, imipramine reduced the uptake of [3H]norepinephrine, decreased the formation of 3,4-[3H]dihydroxymandelic acid, and increased the formation of [3H]normetanephrine. Moreover, cyclazocine increased the formation of endogenous 3-methoxy-4-hydroxyphenylethylene glycol and produced a fall in endogenous norepinephrine. It is suggested that cyclazocine reduces the accumulation of [3H]norepinephrine, decreases endogenous norepinephrine levels, and increases the formation of 3-methoxy-4-hydroxyphenylethylene glycol by interacting with brain adrenergic nerves, presumably by inhibiting neuronal uptake and facilitating norepinephrine turnover.
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