COMPARISON OF THE EFFECTS OF THE ISOMERS OF AMPHETAMINE, METHYLPHENIDATE AND DEOXYPIPRADROL ON THE UPTAKE OF NOREPINEPHRINE-H-3 AND [DOPAMINE-H-3 BY SYNAPTIC VESICLES FROM RAT WHOLE BRAIN, STRIATUM AND HYPOTHALAMUS

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  • 1 January 1979
    • journal article
    • research article
    • Vol. 210  (3) , 422-428
Abstract
The ATP-Mg2+-dependent uptake of [3H]dopamine and l-[3H]norepinephrine into purified synaptic vesicles of whole rat brain, rat striatum and rat hypothalamus was inhibited 10-fold more effectively by S-(+)-amphetamine as compared to its corresponding R-(-)-enantiomer. S-(+)-deoxypipradrol and its R-(-)-enantiomer were approximately equipotent inhibitors of 3H-amine uptake into these synaptic vesicular preparations. The 1R:2R-methylphenidate was 2 times as potent as its 1R:2S-enantiomer as an inhibitor of 3H-catecholamine uptake. The receptor sites on the amine pumps present in the membranes of all 3 vesicles preparations are apparently similar in so far as they are all sensitive to the stereochemical configuration around the .alpha.-carbon of amphetamine but are not sensitive to the stereochemical configuration around the analogous carbon of deoxypipradrol and methylphenidate. These observations are the reverse of those previously observed for the phenethylamine pumps present in peripheral and central neuronal membranes.