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催眠药三唑仑和唑吡坦在整个大脑中具有相同的代谢作用:对苯二氮䓬受体亚型的影响。

The hypnotics triazolam and zolpidem have identical metabolic effects throughout the brain: implications for benzodiazepine receptor subtypes.

作者信息

Piercey M F, Hoffmann W E, Cooper M

机构信息

Upjohn Company, Kalamazoo, MI 49001.

出版信息

Brain Res. 1991 Jul 19;554(1-2):244-52. doi: 10.1016/0006-8993(91)90196-3.

Abstract

Using Sokoloff's 2-deoxyglucose autoradiography procedure, the effects of trizolam, a classical benzodiazepine (BZ) hypnotic, were compared to those of zolpidem, which preferentially binds to BZ1 receptor subtypes. Triazolam depressed metabolism in 40 of the more than 60 brain regions evaluated. Zolpidem depressed metabolism in all of these areas, including the spinal cord, an area where the BZ1 receptor subtype is not supposed to exist. Zolpidem and triazolam also depressed metabolism in the molecular layer of the dentate gyrus, an area low in BZ1 receptors. Neither drug affected metabolism in 21 areas, including the regions most specific for the BZ1 subtype (cerebellum, inferior colliculus, globus pallidus, and substantia nigra pars reticularis). It is concluded that: (i) zolpidem and triazolam depress energy metabolism of the same areas of the brain, (ii) zolpidem's effects may not be mediated solely through the BZ1 receptor subtype, and (iii) the BZ2 receptor may be functionally more significant than the BZ1 receptor.

摘要

采用索科洛夫的2-脱氧葡萄糖放射自显影术,将经典苯二氮䓬(BZ)催眠药三唑仑的作用与优先结合BZ1受体亚型的唑吡坦的作用进行了比较。在评估的60多个脑区中,三唑仑使40个脑区的代谢受到抑制。唑吡坦使所有这些区域的代谢受到抑制,包括脊髓,而脊髓被认为不存在BZ1受体亚型。唑吡坦和三唑仑还使齿状回分子层的代谢受到抑制,该区域BZ1受体含量较低。两种药物对包括对BZ1亚型最具特异性的区域(小脑、下丘、苍白球和黑质网状部)在内的21个区域的代谢均无影响。得出以下结论:(i)唑吡坦和三唑仑抑制大脑相同区域的能量代谢;(ii)唑吡坦的作用可能并非仅通过BZ1受体亚型介导;(iii)BZ2受体在功能上可能比BZ1受体更重要。

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