The influence of the antidepressant pirlindole and its dehydro-derivative on the activity of monoamine oxidase A and GABAA receptor binding.

Autor: Medvedev AE; Institute of Biomedical Chemistry, Russian Academy of Medical Sciences, Moscow, Russia., Shvedov VI, Chulkova TM, Fedotova OA, Saederup E, Squires RF
Jazyk: angličtina
Zdroj: Journal of neural transmission. Supplementum [J Neural Transm Suppl] 1998; Vol. 52, pp. 337-42.
DOI: 10.1007/978-3-7091-6499-0_36
Abstrakt: The influence of pirlindole and dehydro-pirlindole on GABAA receptor binding and MAO-A activity was investigated in vitro. Inhibition of rat brain and human placenta MAO-A by both compounds was much more potent (with IC50 range 0.3-0.005 microM) than that of GABAA receptors. Pirlindole was inactive as a GABA antagonist. Dehydro-pirlindole exhibited selective blockade of GABA-A receptors with EC50 12 microM. Effects of both compounds on MAO-A activity were partially reversible. Data obtained suggest that in contrast to pirlindole dehydro-pirlindole may act not only as a MAO-A inhibitor but also as a potent GABAA receptor blocker.
Databáze: MEDLINE