PMID: 8953568Dec 1, 1996Paper

Effects of the antidepressant pirlindole and its dehydro-derivative on the activity of monoamine oxidase-A and on GABAA receptors

Neurochemical Research
A E MedvedevR F Squires

Abstract

The effects of pirlindole and dehydro-pirlindole on GABAA receptors and MAO-A activity were investigated in vitro. Pirlindole was inactive as a GABA antagonist. Dehydro-pirlindole exhibited partial and selective blockade of a subset of GABAA receptors with an EC50 of 12 microM and maximum reversal (delta Bopt) of 42%. Inhibition of rat brain and human placenta MAO-A by both compounds was much more potent (with IC50 range 0.3-0.005 microM). Their effects on MAO-A activity were partially reversible in vitro. In contrast to pirlindole, dehydro-pirlindole may act not only as MAO-A inhibitor but also as a clozapine-like selective GABAA receptor blocker, preferentially blocking a subset of GABAA receptors that are not sensitive to DMCM or Ro 5-4864.

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Citations

Nov 5, 2003·Clinical Immunology : the Official Journal of the Clinical Immunology Society·M D'EliaJ Bernier
Jan 31, 2013·Journal of Medicinal Chemistry·F Ivy Carroll, William A Carlezon
Sep 1, 2011·Clinical Drug Investigation·Jaime C BrancoAugusto Filipe
Dec 10, 1998·Journal of Chemical Information and Computer Sciences·A E MedvedevA S Ivanov

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