Evoniuk G E, Hertzman R P, Skolnick P
Laboratory of Neuroscience, NIDDK-LN, National Institutes of Health, Bethesda, MD 20892.
Psychopharmacology (Berl). 1991;105(1):125-8. doi: 10.1007/BF02316874.
A simple and rapid method for detecting the behavioral effects of phencyclidine and related dissociative anesthetics is described. Dissociative anesthetics such as phencyclidine (PCP) and dizolcipine, which bind with high affinities at N-methyl-D-aspartate (NMDA) coupled cation channels ("PCP receptors"), produced a dose-related increase in the percentage of mice that fell from a 1.5 cm deep circular arena mounted on a 60 cm platform. A similar behavior was not manifest by other classes of compounds examined including competitive NMDA antagonists, an antagonist at strychnine-insensitive glycine receptors, and sigma-receptor ligands with moderate to low affinities for PCP receptors. Pretreatment of mice with glycine reduced in a dose-dependent manner the percentage of falls elicited by a maximally effective dose of dizolcipine. This simple procedure may prove useful for both the rapid detection of dissociative anesthetics and evaluation of putative PCP antagonists.
本文描述了一种检测苯环利定及相关分离麻醉剂行为效应的简单快速方法。分离麻醉剂如苯环利定（PCP）和地佐环平，它们以高亲和力结合于N-甲基-D-天冬氨酸（NMDA）偶联阳离子通道（“PCP受体”），使置于60厘米高平台上、深1.5厘米圆形场地中的小鼠跌落百分比呈剂量依赖性增加。所检测的其他类化合物，包括竞争性NMDA拮抗剂、士的宁不敏感甘氨酸受体拮抗剂以及对PCP受体具有中度至低度亲和力的σ受体配体，均未表现出类似行为。用甘氨酸预处理小鼠可剂量依赖性降低最大有效剂量地佐环平引起的跌落百分比。这一简单程序可能对快速检测分离麻醉剂及评估推定的PCP拮抗剂均有用。
