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Synthesis and Anxiolytic Activity of 9-(4-Ethylpiperazino-1-Carbonyl)Fluoren-9-OL Hydrochloride, A Structural Analog of the M-Choline Blocker Amizil
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2021-07-22 , DOI: 10.1007/s11094-021-02423-y
L. K. Khnychenko 1 , E. E. Yakovleva 1 , V. E. Gmiro 1 , P. D. Shabanov 1
Affiliation  

Experiments on rats in a depressive-like state model caused by reserpine employed the elevated plus-maze and open-field tests and showed that 9-(4-ethylpiperazino-1-carbonyl)fluoren-9-ol hydrochloride, a structural analog of the M-choline blocker amizil, at a dose of 10 mg/kg (1/16 LD50) in an intraperitoneal administration course (30 d) had an anxiolytic effect, stimulated exploratory activity, and normalized the vegetative reactions of experimental animals. The strength of the anxiolytic effect of this compound was comparable to that of the benzodiazepine anxiolytic diazepam. Statistically significant differences in the numbers of visits to the open and closed arms and the times spent in those arms in the elevated-plus maze test after administration of the test compound or diazepam were not found. The obtained results indicate that the structural analog of amizil is promising for development as a drug producing an anxiolytic effect in neurotic states to eliminate emotional instability.



中文翻译:

9-(4-Ethylpiperazino-1-Carbonyl) Fluoren-9-OL 盐酸盐的合成和抗焦虑活性,M-胆碱阻滞剂 Amizil 的结构类似物

对处于由利血平引起的抑郁样状态模型的大鼠进行的实验采用高架十字迷宫和开放场试验,结果表明 9-(4-乙基哌嗪-1-羰基)芴-9-醇盐酸盐,其结构类似物M-胆碱阻滞剂amizil,剂量为10 mg/kg (1/16 LD 50) 在腹腔给药过程中 (30 d) 具有抗焦虑作用,刺激探索活动,并使实验动物的植物反应正常化。该化合物的抗焦虑作用强度与苯二氮卓类抗焦虑药地西泮相当。未发现在给予测试化合物或地西泮后,在高架十字迷宫试验中,打开和闭合臂的访问次数以及在这些臂中花费的时间的统计学显着差异。获得的结果表明,amizil 的结构类似物有望开发为一种在神经症状态下产生抗焦虑作用以消除情绪不稳定的药物。

更新日期:2021-07-22
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