2,3,3a,4,5,6-Hexahydro-8-methyl-1H-pyrazino[3,2,1-j,k]carbazole mesylate

Description

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 (K_is = 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.

Uses

Antidepressive;Monoamine oxidase inhibitor

Biological Activity

A highly selective reversible inhibitor of monoamine oxidase type A.

References

[1] J. BRUHWYLER  J. G  J F LIéGEOIS. PIRLINDOLE: A SELECTIVE REVERSIBLE INHIBITOR OF MONOAMINE OXIDASE A. A REVIEW OF ITS PRECLINICAL PROPERTIES[J]. Pharmacological research, 1997, 36 1: Pages 23-33. DOI: 10.1006/phrs.1997.0196
[2] MóNICA MORAIS. The effects of chronic stress on hippocampal adult neurogenesis and dendritic plasticity are reversed by selective MAO-A inhibition.[J]. Journal of Psychopharmacology, 2014, 28 12: 1178-1183. DOI: 10.1177/0269881114553646
[3] RACHEL ULFERTS. Screening of a Library of FDA-Approved Drugs Identifies Several Enterovirus Replication Inhibitors That Target Viral Protein 2C[J]. Antimicrobial Agents and Chemotherapy, 2016, 60 1: 2627-2638. DOI: 10.1128/aac.02182-15