Effects of tranylcypromine enantiomers on monoamine uptake and release and imipramine binding

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Abstract
Studies were carried outin vitro to determine effects of tranylcypromine enantiomers ([+]- and [−]-TCP) on uptake and release of 5-HT, DA and NA in rat synaptosomes and on imipramine binding to rabbit platelets. (+)-TCP was more potent than (−)-TCP as inhibitor of 5-HT uptake and imipramine binding, whereas (−)-TCP was more potent than (+)-TCP as inhibitor of DA and NA uptake. The enantiomers differed only slightly in their effects on monoamine release. The findings agree with previous reports on the stereoselectivity of monoaminergic mechanisms toward TCP enantiomers, and support the notion that the 5-HT uptake site may be associated with the imipramine binding site.