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一种基于苯二氮䓬类药物阻断小鼠中γ-氨基丁酸诱导的肌阵挛性抽搐能力的评估新方法。

A new method for the evaluation of benzodiazepines based on their ability to block muscimol-induced myoclonic jerks in mice.

作者信息

Menon M K, Vivonia C A, Haddox V G

出版信息

Psychopharmacology (Berl). 1981;75(3):291-3. doi: 10.1007/BF00432441.

Abstract

A number of clinically used benzodiazepines were tested for their effectiveness in blocking muscimol-induced myoclonic jerks in mice. Their ED50 values were determined from their dose-response curves. These data gave the following relative potencies with respect to diazepam: diazepam = 1, medazepam = 0.24, oxazepam = 1.27, flurazepam = 1.90, lorazepam = 3.01, nitrazepam = 3.93, clonazepam = 33.14, and flunitrazepam = 116.00. Because our earlier studies indicated that muscimol-induced myoclonic jerks probably originate from the spinal cord, the present method may prove to be suitable for quantitatively evaluating the effect of benzodiazepines on the spinal cord. The present results also indicate the possible value of flunitrazepam in the management of neurologic disorders in which preferential action on the spinal cord is desired.

摘要

对一些临床使用的苯二氮䓬类药物进行了测试,以考察它们阻断小鼠中由蝇蕈醇诱导的肌阵挛性抽搐的有效性。根据其剂量反应曲线确定了它们的半数有效剂量(ED50)值。这些数据得出了以下相对于地西泮的相对效价:地西泮 = 1,美达西泮 = 0.24,奥沙西泮 = 1.27,氟西泮 = 1.90,劳拉西泮 = 3.01,硝西泮 = 3.93,氯硝西泮 = 33.14,氟硝西泮 = 116.00。由于我们早期的研究表明,蝇蕈醇诱导的肌阵挛性抽搐可能起源于脊髓,因此本方法可能被证明适用于定量评估苯二氮䓬类药物对脊髓的作用。目前的结果还表明,氟硝西泮在治疗希望对脊髓有优先作用的神经疾病方面可能具有价值。

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