抗抑郁药匹克隆及其脱氢衍生物对单胺氧化酶A活性和γ-氨基丁酸A型（GABAA）受体结合的影响。

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

作者信息

Medvedev A E, Shvedov V I, Chulkova T M, Fedotova O A, Saederup E, Squires R F

机构信息

Institute of Biomedical Chemistry, Russian Academy of Medical Sciences, Moscow, Russia.

出版信息

J Neural Transm Suppl. 1998;52:337-42. doi: 10.1007/978-3-7091-6499-0_36.

DOI:10.1007/978-3-7091-6499-0_36

PMID:9564636

Abstract

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.

摘要

在体外研究了匹克隆朵和脱氢匹克隆朵对GABAA受体结合及单胺氧化酶A（MAO-A）活性的影响。两种化合物对大鼠脑和人胎盘MAO-A的抑制作用比其对GABAA受体的抑制作用更强效（IC50范围为0.3 - 0.005微摩尔）。匹克隆朵作为GABA拮抗剂无活性。脱氢匹克隆朵对GABA-A受体表现出选择性阻断作用，其半数有效浓度（EC50）为12微摩尔。两种化合物对MAO-A活性的影响部分是可逆的。所获得的数据表明，与匹克隆朵不同，脱氢匹克隆朵不仅可能作为MAO-A抑制剂起作用，还可能作为一种强效的GABAA受体阻断剂起作用。