Biological Activity
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 (IC50s = 250 and 34.2 nM for rat brain and heart MAO-A, respectively).1 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.2 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.3
References
1.Bruhwyler, J., Liégeois, J.F., and Géczy, J.Pirlindole: A selective reversible inhibitor of monoamine oxidase A. A review of its preclinical propertiesPharmacol. Res.36(1)23-33(1997)
2.Morais, M., Santos, P.A., Mateus-Pinheiro, A., et al.The effects of chronic stress on hippocampal adult neurogenesis and dendritic plasticity are reversed by selective MAO-A inhibitionJ. Psychopharmacol.28(12)1178-1183(2014)
3.Ulferts, R., de Boer, S.M., van der Linden, L., et al.Screening of a library of FDA-approved drugs identifies several enterovirus replication inhibitors that target viral protein 2CAntimicrob. Agents Chemother.60(5)2627-2638(2016)
