Antidepressant profile of bupropion
and three metabolites in mice

Martin P, Massol J, Colin JN, Lacomblez L, Puech AJ
Departement de Pharmacologie,
Faculte de Medicine Pite-Salpetriere, Paris,
Pharmacopsychiatry 1990 Jul; 23(4):187-94


Bupropion is a novel antidepressant, distinct from tricyclic antidepressants both neurochemically and behaviorally. Bupropion forms several metabolites in both rodents and humans. Three chemically different molecules - BW 306, BW 494, and BW 287 - were selected. Comparative assessment of antidepressant activity of bupropion and its metabolites in mice, and pharmacological analysis of possible mechanisms of action of the parent drug and its metabolites (using interaction studies with pimozide, D,L-propranolol, and prazosin) were carried out. The results obtained show that: bupropion has a pharmacological spectrum in various animal models which predicts both antidepressant and stimulatory activity in man. BW 306 is the most active of the metabolites studied and, compared to bupropion, seems more "antidepressant" and less stimulant. BW 494, compared to bupropion or BW 306, has a lower degree of activity in various tests used to evaluate antidepressants. BW 287 has no effect in any of the tests used in this study. The interaction studies with pimozide, D,L-propranolol, and prazosin in the various tests have shown that: the stimulatory effect of bupropion, BW 306, and BW 494 is antagonized by both pimozide and prazosin. in the behavioral despair test, the reduction in the duration of immobility by bupropion and BW 494 is antagonized by pimozide, but not by prazosin or D,L-propranolol. the antagonism of reserpine-induced hypothermia by bupropion and BW 306 is significantly decreased by prazosin and D,L-propranolol, but not by pimozide. These data suggest that the clinical antidepressant profile (without a major stimulatory effect) observed in man after administration of bupropion is related to metabolite BW 306 and possibly to BW 494, rather than to bupropion itself.
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Bupropion and REM sleep
Hypersomnia and depression
Bupropion for nicotine quitters
Bupropion (Wellbutrin) vs SSRIs
Bupropion for depressed bipolars
Bupropion used to augment SSRIs
Bupropion, noradrenaline and serotonin
Bupropion for ADHD and bipolar disorder
Bupropion and the dopamine transporter
Bupropion and psychomotor performance
Bupropion (Wellbutrin) for major depressive disorder
Bupropion (Wellbutrin): prescribing information (PDF)

and further reading

Future Opioids
BLTC Research
Utopian Surgery?
The Abolitionist Project
The Hedonistic Imperative
The Reproductive Revolution
Critique of Huxley's Brave New World

The Good Drug Guide
The Good Drug Guide

The Responsible Parent's Guide
To Healthy Mood Boosters For All The Family