Para-substituted amphetamines and brain serotonin.
Among the para-substituted amphetamines was V-111 the most potent inhibiting of examined synaptosomal reuptake of 3H-5-HT. In this respect both optical isomers of V-111 were equally effective while in the inhibition of the uptake of 3H-NA and mainly in that of 3H-DA the (+) form was found to be more potent inhibitor. Concerning the releasing potency of the former amines, in the case of 3H-5-HT both isomers were equally effective releasers. The release of 3H-NA and 3H-DA was influenced more effectively by the (+) form. The stereoselective influence of V-111 on the amine reuptake and release suggests a possibility to reach more selective serotonergic and catecholaminergic effects of amphetamines. For the irreversible inhibition of the uptake in vivo presumably one of the metabolities of V-111 is responsible.
D000818:Animals; D001921:Brain / Q000378:metabolism* / Q000648:ultrastructure; D003864:Depression, Chemical; D004298:Dopamine / Q000378:metabolism; D066298:In Vitro Techniques; D008694:Methamphetamine / Q000031:analogs & derivatives* / Q000494:pharmacology; D009638:Norepinephrine / Q000378:metabolism; D051381:Rats; D012701:Serotonin / Q000378:metabolism*; D013237:Stereoisomerism; D013574:Synaptosomes / Q000378:metabolism*
D012701:Serotonin; D008694:Methamphetamine; D004298:Dopamine; D009638:Norepinephrine