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吗氯贝胺对大鼠脑单胺氧化酶A和B的影响:与骆驼蓬碱和氯吉兰的比较。

Effect of moclobemide on rat brain monoamine oxidase A and B: comparison with harmaline and clorgyline.

作者信息

Gerardy J

机构信息

Department of Pharmacology, University of Liège, Sart Tilman, Belgium.

出版信息

Prog Neuropsychopharmacol Biol Psychiatry. 1994 Jul;18(4):793-802. doi: 10.1016/0278-5846(94)90085-x.

Abstract
  1. Effects of moclobemide (12.5, 25 and 50 mg/kg), harmaline (10 mg/kg) and clorgyline (10 mg/kg) on monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B) were examined ex vivo by a fluorometric method with tyramine (T) and phenylethylamine (PEA) as substrates. Six rat brain areas were dissected for this purpose. 2. Moclobemide had decreased MAO-A activity in all areas examined by a dose-dependent manner; the largest decrease was observed in tuberculum olfactorium and striatum. MAO-B activity after moclobemide had presented some dose-dependently inhibition (about 30 percent at a dose of 50 mg/kg). 3. Harmaline was more potent than moclobemide as MAO-A inhibitor but had left MAO-B activity unchanged. 4. Clorgyline was the most potent of the three drug tested for MAO-A inhibition. MAO-B activity was inhibited at the dose used in these experiments. 5. MAO-A inhibitory properties on tuberculum olfactorium and striatum could be of interest according to some animal models of depression.
摘要
  1. 采用荧光法,以酪胺(T)和苯乙胺(PEA)为底物,离体检测吗氯贝胺(12.5、25和50毫克/千克)、骆驼蓬碱(10毫克/千克)和氯吉兰(10毫克/千克)对单胺氧化酶A(MAO-A)和单胺氧化酶B(MAO-B)的影响。为此解剖了六个大鼠脑区。2. 吗氯贝胺以剂量依赖方式降低了所有检测区域的MAO-A活性;在嗅结节和纹状体中观察到最大降幅。吗氯贝胺作用后的MAO-B活性呈现出一定的剂量依赖性抑制(50毫克/千克剂量时约为30%)。3. 作为MAO-A抑制剂,骆驼蓬碱比吗氯贝胺更有效,但对MAO-B活性无影响。4. 氯吉兰是所测试的三种药物中对MAO-A抑制作用最强的。在这些实验所用剂量下,MAO-B活性受到抑制。5. 根据一些抑郁症动物模型,MAO-A对嗅结节和纹状体的抑制特性可能值得关注。

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