Effects of tranylcypromine enantiomers on monoamine uptake and release and imipramine binding.
Studies were carried out in 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 stereo-selectivity of monoaminergic mechanisms toward TCP enantiomers, and support the notion that the 5-HT uptake site may be associated with the imipramine binding site.
Tuomisto
J
J
Smith
D F
DF
D000588:Amines / Q000378:metabolism*; D000818:Animals; D001665:Binding Sites; D001693:Biological Transport, Active / Q000187:drug effects; D001792:Blood Platelets / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism; D007099:Imipramine / Q000378:metabolism*; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D009638:Norepinephrine / Q000378:metabolism; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012701:Serotonin / Q000378:metabolism; D013237:Stereoisomerism; D013574:Synaptosomes / Q000378:metabolism; D014191:Tranylcypromine / Q000494:pharmacology*
D000588:Amines; D012701:Serotonin; D014191:Tranylcypromine; D007099:Imipramine; D004298:Dopamine; D009638:Norepinephrine