Cyamemazine的临床前和临床药理学:抗焦虑作用和预防酒精和苯二氮卓戒断综合征

Michel Bourin, Eric Dailly, Martine Hascöet
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引用次数: 30

摘要

几项研究表明,抗精神病化合物氰胺嗪对人类具有抗焦虑的特性。通过结合、微透析和行为研究建立的cyamemazine (D2、5-HT2A、5-HT2C和5-HT3受体拮抗剂)的原始药理谱与这些观察结果一致。在光/暗探索试验中,氰胺嗪在急性给药时表现出抗焦虑样活性,而不是慢性给药。然而,通过长期给药,氰胺嗪增加了在高水平迷宫(EPM)测试中张开双臂的时间,显示出抗焦虑样活性。急性和慢性给药在这些试验中获得的结果之间的差异可能是由于多巴胺D2受体拮抗剂与5-HT2C和5-HT3受体拮抗剂的结合。氰胺嗪对多巴胺能系统和5-HT3受体的作用也可以解释临床前研究中证明的氰胺嗪在酒精戒断治疗中的活性。最近在临床试验中对氰胺嗪的潜在适应症及其在苯二氮卓类戒断综合征中的活性进行了研究,并在本文中介绍了这些研究的结果。
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Preclinical and Clinical Pharmacology of Cyamemazine: Anxiolytic Effects and Prevention of Alcohol and Benzodiazepine Withdrawal Syndrome

Several studies have suggested that the antipsychotic compound, cyamemazine, possesses anxiolytic properties in humans. The original pharmacological profile of cyamemazine (D2, 5-HT2A, 5-HT2C, and 5-HT3 receptor antagonist), which was established by binding, microdialysis and behavioral studies, is consistent with these observations. In the light/dark exploration test, cyamemazine demonstrated anxiolytic-like activity by acute, but not chronic administration. By chronic administration, however, cyamemazine increased the time spent in the open arms of the elevated plus maze (EPM) test demonstrating anxiolytic-like activity. The discrepancy between the results obtained in these tests by acute and chronic administration, could be due to a combination of dopamine D2 receptor antagonism with antagonism of the 5-HT2C and 5-HT3 receptors. The action of cyamemazine on both the dopaminergic system and 5-HT3 receptors could also explain the activity of cyamemazine in the management of alcohol withdrawal demonstrated in preclinical studies. This potential indication for cyamemazine and its activity in benzodiazepine withdrawal syndrome have recently been investigated in clinical trials and the results of these studies are presented in this review.

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