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Pseudophenmetrazine

Pseudophenmetrazine is a psychostimulant compound of the morpholine class. It is the N- demethylated and cis- configured analogue of phendimetrazine as well as the cis-configured stereoisomer of phenmetrazine. In addition, along with phenmetrazine, it is believed to be one of the active metabolites of phendimetrazine, which itself is inactive and behaves merely as a prodrug. Relative to phenmetrazine, pseudophenmetrazine is of fairly low potency, acting as a modest releasing agent of norepinephrine ( EC = 514 nM), while its - enantiomer is a weak releaser of dopamine (EC = 1,457 nM) whereas its -enantiomer is a weak reuptake inhibitor of dopamine (K = 2,691 nM); together as a racemic mixture with the two enantiomers combined, pseudophenmetrazine behaves overall more as a dopamine reuptake inhibitor (K = 2,630 nM), possibly due to the -enantiomer blocking the uptake of the -enantiomer into dopaminergic neurons and thus preventing it from inducing dopamine release. Neither enantiomer has any significant effect on serotonin reuptake or release (both K = >10,000 nM and EC = >10,000 nM, respectively).