Evidence that the reversible MAO-A inhibitor moclobemide increases prolactin secretion by a serotonergic mechanism in healthy male volunteers.

Abstract The serotonin receptor antagonist methysergide was used to investigate the mechanism mediating stimulation of prolactin release after single doses of the reversible MAO-A inhibitor moclobemide. Eight healthy male volunteers participated in a placebo-controlled cross-over study, where pretreatment with methysergide almost totally prevented the moclobemide-induced increase in plasma prolactin levels. MAO-A inhibition, as evidenced by up to 80% decreases in the plasma concentration of 3, 4-dihydroxyphenylglycol, a deaminated metabolite of norepinephrine, was similar after both pretreatments. This result suggests that moclobemide stimulates prolactin release through activation of serotonergic receptors, and provides evidence that the drug is capable of augmenting central serotonergic neurotransmission in humans.