Abstract

Synaptosomes from whole brain of rats accumulated serotonin by means of a high affinity process and a low affinity process, distinguishable kinetically. The high affinity process was stronly inhibited by 4-chloroamphetamine. 3-Chloroamphetamine, 2-chloroamphetamine and amphetamine were progressively weaker inhibitors of that process. 4-Chloroamphetamine was a less potent inhibitor of the low affinity process (about equal to amphetamine). When 4-chloroamphetamine was administered to rats and synaptosomes were isolated from whole brain, the high affinity uptake of serotonin was inhibited for as long as 22·5 hr after drug administration. In vitro, 4-chloroamphetamine but not chloroimipramine at 5 μM caused a release of serotonin from synaptosomes preincubated with radioactive serotonin. The ability of 4-chloroamphetamine to inhibit the high affinity uptake of serotonin by synaptosomes and to release serotonin from synaptosomes is probably related to the prolonged lowering of brain serotonin levels in rats treated with 4-chloroamphetamine.

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