pirlindole mesylate

monoamine oxidase type A inhibitor

Pirlindole, a reversible inhibitor of monoamine oxidase A (RIMA), has been developed and used primarily as an antidepressant compound in Russia. Structurally and pharmacologically, it is similar to metralindole. Pirlindole has received approval for the treatment of depression in several European and non-European countries. Its oral absolute bioavailability ranges from 20% to 30%, mainly due to significant first-pass metabolism. In rats, the oral Tmax varies between 2.5 and 6 hours, while in dogs, it ranges from 0.8 to 2 hours.

Pirlindole, a reversible inhibitor of monoamine oxidase A (RIMA), was developed and is used as an antidepressant in Russia. It is structurally and pharmacologically related to metralindole. Pirlindole has been approved for the treatment of depression in several European and non-European countries. Due to extensive first-pass effects, its absolute bioavailability ranges from 20% to 30%. When administered orally, the Tmax in rats varies from 2.5 to 6 hours, while in dogs it ranges from 0.8 to 2 hours.

Pirlindole-d4 is intended for use as an internal standard for the quantification of pirlindole by GC- or LC-MS. Pirlindole is a selective and reversible monoamine oxidase A (MAO-A) inhibitor. It is selective for MAO-A over MAO-B. 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.

Pirlindole is a reversible inhibitor of monoamine oxidase A (RIMA). It is structurally and pharmacologically related to metralindole.