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 |
Externí odkaz: |
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