BROFAROMINE - A MONOAMINE OXIDASE-A AND SEROTONIN UPTAKE INHIBITOR

Brofaromine is a tight-binding, reversible inhibitor of monoamine oxid ase-A (MAO-A), with concomitant serotonin (5-HT) uptake-inhibiting pro perties. In psychopharmacologic investigations, the compound shows the properties expected of an MAO inhibitor, antagonizing the effects of reserpine, tetrabenazine, and 5-hydroxytryptophan in rats and mice, an d suppressing rapid eye movement sleep in cats. Brofaromine showed ant idepressant-like activity in a rat social conflict test. In radioligan d binding assays, brofaromine exhibited weak or no interaction with al pha1- and alpha2-noradrenergic, 5-HT1, 5-HT2, 5-HT3, cholinergic, hist amine H-1 and H-2, /mu-opiate, GABA(A), benzodiazepine, adenosine, neu rotensin, and substance P receptors. Comparison of in vitro and in viv o potencies to inhibit 5-HT uptake with those of reference drugs, and direct evidence in patients and volunteers suggest that 5-HT uptake in hibition plays a role in the clinical profile of brofaromine.