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环吡咯酮类药物的药理及临床研究:佐匹克隆与舒里克隆

Pharmacological and clinical studies of cyclopyrrolones: zopiclone and suriclone.

作者信息

Julou L, Blanchard J C, Dreyfus J F

出版信息

Pharmacol Biochem Behav. 1985 Oct;23(4):653-9. doi: 10.1016/0091-3057(85)90433-2.

Abstract

Among the non-benzodiazepine compounds which have been found to interact with the "GABA receptor-BZ receptor-chloride channel complex," the very chemically original cyclopyrrolone family has a special place. This has been demonstrated using selected pharmacological, biochemical and clinical data obtained with two cyclopyrrolones, zopiclone and suriclone, which, in addition to their capacity of displacing BZ from their sites, simultaneously possess the main pharmacological properties of BZ and well established therapeutic activities, as hypnotic and anxiolytic, respectively. However, although cyclopyrrolones recognize BZ receptor sites, their mechanism of action might not exactly fit with that of BZ. Indeed, using tritiated zopiclone and suriclone, it has been shown that they could act on sites distinct from those of BZ or could induce receptor conformational changes different from those induced by BZ.

摘要

在已发现与“γ-氨基丁酸(GABA)受体-苯二氮䓬(BZ)受体-氯离子通道复合物”相互作用的非苯二氮䓬类化合物中,化学结构非常独特的环吡咯酮家族占有特殊地位。这一点已通过使用两种环吡咯酮(佐匹克隆和舒立克隆)获得的选定药理学、生物化学和临床数据得到证明,这两种环吡咯酮除了具有将苯二氮䓬从其位点置换出来的能力外,还同时具备苯二氮䓬的主要药理学特性以及已确立的治疗活性,分别为催眠和抗焦虑作用。然而,尽管环吡咯酮能识别苯二氮䓬受体位点,但其作用机制可能与苯二氮䓬并不完全相同。实际上,使用氚标记的佐匹克隆和舒立克隆已表明,它们可能作用于与苯二氮䓬不同的位点,或者诱导与苯二氮䓬诱导的不同的受体构象变化。

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