Pre-clinical Pharmacology of Moclobemide

The novel antidepressant, moclobemide, is a reversible inhibitor of monoamine oxidase (MAO) preferentially of monoamine oxidise-A (MAO-A); it emerged for study out of a series of lipid-lowering agents. In spite of its weak MAO-A inhibition in vitro, moclobemide is a potent inhibitor of MAO-A, in vivo; its in vivo activity is of short duration, in contrast to the extremely long-lasting inhibition, e.g. by tranylcypromine. Moclobemide only slightly potentiates the pressor effect of oral tyramine in freely moving rats, again in contrast to tranylcypromine; it is not anti-cholinergic and is free of hepatotoxicity. Published evidence on the preclinical pharmacology is reviewed.