Biological activity

bioactivebiologically activebioactivity

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.

Potency (pharmacology)

potentpotencypotencies

Relative to phenmetrazine, pseudophenmetrazine is of fairly low potency, acting as a modest releasing agent of norepinephrine (EC 50 = 514 nM), while its -enantiomer is a weak releaser of dopamine (EC 50 = 1,457 nM) whereas its -enantiomer is a weak reuptake inhibitor of dopamine (K i = 2,691 nM); together as a racemic mixture with the two enantiomers combined, pseudophenmetrazine behaves overall more as a dopamine reuptake inhibitor (K i = 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.

EC50

EC 50 EC 50pEC 50

Relative to phenmetrazine, pseudophenmetrazine is of fairly low potency, acting as a modest releasing agent of norepinephrine (EC 50 = 514 nM), while its -enantiomer is a weak releaser of dopamine (EC 50 = 1,457 nM) whereas its -enantiomer is a weak reuptake inhibitor of dopamine (K i = 2,691 nM); together as a racemic mixture with the two enantiomers combined, pseudophenmetrazine behaves overall more as a dopamine reuptake inhibitor (K i = 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.

Reuptake inhibitor

inhibitinhibitorinhibiting

Relative to phenmetrazine, pseudophenmetrazine is of fairly low potency, acting as a modest releasing agent of norepinephrine (EC 50 = 514 nM), while its -enantiomer is a weak releaser of dopamine (EC 50 = 1,457 nM) whereas its -enantiomer is a weak reuptake inhibitor of dopamine (K i = 2,691 nM); together as a racemic mixture with the two enantiomers combined, pseudophenmetrazine behaves overall more as a dopamine reuptake inhibitor (K i = 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.