BIOCHEMICAL PHARMACOLOGY OF BEFLOXATONE (MD370503), A NEW POTENT REVERSIBLE MAO-A INHIBITOR

In vitro and ex-vivo studies show that befloxatone, a new oxazolidinon e derivative, is a potent, reversible, competitive and specific MAO-A inhibitor (KiA from 1.9 to 3.6 nM and KiB/KiA ratio between 100 and 40 0, in the Rat and in Man, depending on the tissue). Befloxatone posses ses a marked activity in antidepressant-sensitive behavioral models in rats (from 0.03 to 0.15 mg/kg po) and mice (from 0.21 to 0.29 mg/kg p o). At these doses, befloxatone does not induce a significant potentia tion of oral tyramine. Befloxatone is devoid of sedative, anticholiner gic and cardiovascular effects. Befloxatone is rapidly and extensively distributed in rat brain, the pharmacokinetics are linear in the rat and in man in a large range of doses. Befloxatone is well tolerated in healthy volunteers and is developed as an antidepressant.