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两种立体异构拟精神病性乙醇酸盐的行为效应和结合亲和力。

Behavioral effects and binding affinities of two stereoisomeric psychotomimetic glycolates.

作者信息

Lowy K, Abood L G, Raines H

出版信息

J Neurosci Res. 1976;2(2):157-65. doi: 10.1002/jnr.490020206.

Abstract

A comparison was made of the behavioral effects in cats of the dextro and levo isomers of 3-quinuclidinyl benzilate (QB), using a special computer-controlled program. Such psychophysical parameters as rate of response and tendency to use the left or right paw for lever pressing were used primarily to evaluate drug efficacy. The drug did not alter auditory threshold or the percentage of errors in lever pressing. The l-isomer was found to be at least 100 times as potent as the d-isomer, the effects of both being qualitatively similar. After a single dose of 5 mug/Kg of 1-QB, the cats' performance did not return to normal until 5-7 days later. Pretreatment of the cats with a dose of 2 mg/Kg of atropine, an antimuscarinic agent, did not prevent the behavioral effects of 1-QB. The binding affinity of two isomers for synaptic membranes and phosphatidyl serine was identical.

摘要

使用一个特殊的计算机控制程序,对猫进行了3-喹核醇基苯甲酸酯(QB)右旋和左旋异构体行为效应的比较。主要使用诸如反应速率以及用左爪或右爪按压杠杆的倾向等心理物理学参数来评估药物疗效。该药物未改变听觉阈值或按压杠杆时的错误百分比。发现左旋异构体的效力至少是右旋异构体的100倍,两者的效应在性质上相似。单次给予5微克/千克的左旋QB后,猫的行为表现直到5-7天后才恢复正常。用2毫克/千克的抗毒蕈碱剂阿托品对猫进行预处理,并未阻止左旋QB的行为效应。两种异构体对突触膜和磷脂酰丝氨酸的结合亲和力相同。

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