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新型抗焦虑药物6-(邻氯苯基)-8-乙基-1-甲基-4H-三唑并[3,4-c]噻吩并[2,3-e][1,4]二氮杂卓(Y-7131)的药理特性

Pharmacological properties of 6-(o-chlorophenyl)-8-ethyl-1-methyl-4H-s-triazolo[3,4-c]thieno[2,3-e] [1,4]diazepine (Y-7131), a new anti-anxiety drug.

作者信息

Tsumagari T, Nakajima A, Fukuda T, Shuto S, Kenjo T, Morimoto Y, Takigawa Y

出版信息

Arzneimittelforschung. 1978;28(7):1158-64.

PMID:39570
Abstract

6-(o-Chlorophenyl)-8-ethyl-1-methyl-4H-s-triazolo[3,4-c]thienol[2,3-e][1,4]diazepine (Y-7131), a new derivative of the thienodiazepines, had marked activities in antipentylenetetrazole effect in mice, attenuation of conflict behavior in rats, inhibition of aggressive behavior induced by hypothalamic stimulation in cats and muscle relaxant effects in normal and decerebrate cats. Y-7131 had weak activities in anti-MES effect in mice and loss of righting reflex in mice. The acute toxicity of Y-7131 was considerably lower than that of diazepam. No significant autonomic or neuroleptic effects were noted. Y-7131 appears to be a characteristic and potent anti-anxiety agent different from the benzodiazepines.

摘要

6-(邻氯苯基)-8-乙基-1-甲基-4H-1,2,4-三唑并[3,4-c]噻吩并[2,3-e][1,4]二氮杂卓(Y-7131),一种噻吩并二氮杂卓的新衍生物,在小鼠抗戊四氮效应、减轻大鼠冲突行为、抑制猫下丘脑刺激诱导的攻击行为以及对正常和去大脑猫的肌肉松弛作用方面具有显著活性。Y-7131在小鼠抗最大电休克效应和小鼠翻正反射消失方面活性较弱。Y-7131的急性毒性明显低于地西泮。未观察到明显的自主神经或抗精神病作用。Y-7131似乎是一种不同于苯二氮卓类的具有特征性的强效抗焦虑药物。

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