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Pirlindole is a selective and reversible monoamine oxidase A (MAO-A) inhibitor (IC50s = 250 and 34.2 nM for rat brain and heart MAO-A, respectively). It is selective for MAO-A over MAO-B (Kis = 52,100 and 59,900 nM, for rat brain and heart MAO-B, respectively). In rats, it reverses the depressive-like effects induced by chronic mild stress (CMS), increases proliferation of hippocampal neural progenitor cells, and reverses dendritic atrophy in granule neurons. Pirlindole is also an inhibitor of enterovirus-D68 and coxsackievirus B3 (CV-B3), inhibiting the genome replication phase of CV-B3 infection with an EC50 value of 7.7 µM independent of MAO-A activity.

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