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去甲氯氮卓及其他苯二氮䓬类药物的药理学特性。

The pharmacological profile of chlordesmethyldiazepam and other benzodiazepines.

作者信息

Chojnacka-Wójcik E, Tatarczyńska E, Wiczyńska B, Lewandowska A, Przegaliński E

出版信息

Pol J Pharmacol Pharm. 1986 Mar-Apr;38(2):207-13.

PMID:2875452
Abstract

The pharmacological profile of chlordesmethyldiazepam was studied in mice and compared with that of other benzodiazepines (diazepam, lorazepam, clonazepam, nitrazepam, oxazepam, flunitrazepam, medazepam and chlordiazepoxide). All the drugs were administered perorally and their anticonvulsive activity (antagonism towards pentetrazole-induced clonic convulsions), anxiolytic action (the four-plate test), myorelaxant activity (the rota-rod test), sedative effect (inhibition of the locomotor activity) and neurotoxic effect (abolition of the righting reflex) were estimated. Chlordesmethyldiazepam revealed an anticonvulsive action (ED50 = 0.11 mg/kg), anxiolytic activity (MED = 2 mg/kg), myorelaxant action (ED50 = 17.5 mg/kg), sedative effect (ED50 = 34 mg/kg) and neurotoxic action (NTD50 = 190 mg/kg). Considering the potency of action (ED50) in respective tests and the therapeutic indices (NTD50/ED50 ratio), chlordesmethyldiazepam in respect of its profile resembles most lorazepam and diazepam.

摘要

在小鼠中研究了去甲氯地西泮的药理学特性,并与其他苯二氮䓬类药物(地西泮、劳拉西泮、氯硝西泮、硝西泮、奥沙西泮、氟硝西泮、美达西泮和氯氮卓)进行了比较。所有药物均经口服给药,并评估了它们的抗惊厥活性(对戊四氮诱导的阵挛性惊厥的拮抗作用)、抗焦虑作用(四板试验)、肌松活性(转棒试验)、镇静作用(对运动活性的抑制)和神经毒性作用(翻正反射消失)。去甲氯地西泮显示出抗惊厥作用(半数有效剂量[ED50]=0.11毫克/千克)、抗焦虑活性(最小有效剂量[MED]=2毫克/千克)、肌松作用(ED50=17.5毫克/千克)、镇静作用(ED50=34毫克/千克)和神经毒性作用(半数中毒剂量[NTD50]=190毫克/千克)。考虑到在各个试验中的作用效力(ED50)和治疗指数(NTD50/ED50比值),去甲氯地西泮在其特性方面与劳拉西泮和地西泮最为相似。

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