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MK-801在大鼠中具有苯环己哌啶样辨别刺激特性。

Phencyclidine-like discriminative stimulus properties of MK-801 in rats.

作者信息

Willetts J, Balster R L

机构信息

Department of Pharmacology and Toxicology, Medical College of Virginia, Virginia Commonwealth University, Richmond 23298.

出版信息

Eur J Pharmacol. 1988 Jan 27;146(1):167-9. doi: 10.1016/0014-2999(88)90498-0.

Abstract

The discriminative stimulus properties of the N-methyl-D-aspartate (NMDA) antagonist MK-801 ((+)-5-methyl-10,11-dihydro-5H-dibenzo(a,d)cyclohepten-5,10-imine) were investigated in rats trained to discriminate phencyclidine (PCP; 1.25 mg/kg i.p.) from saline on a standard two-lever fixed ratio 32 schedule of food reinforcement. MK-801 was generalized from PCP in a dose-dependent manner, with an ED50 of 0.10 mg/kg i.p. The ED50 for PCP was 0.7 mg/kg io.p. MK-801 is, therefore, a very potent PCP-like drug which may share cellular mechanisms and other effects with PCP, including the antagonism of NMDA.

摘要

在训练大鼠按照标准的双杠杆固定比率32食物强化程序区分苯环利定(PCP;腹腔注射1.25毫克/千克)和生理盐水的实验中,对N-甲基-D-天冬氨酸(NMDA)拮抗剂MK-801((+)-5-甲基-10,11-二氢-5H-二苯并(a,d)环庚烯-5,10-亚胺)的辨别刺激特性进行了研究。MK-801以剂量依赖的方式从PCP泛化,腹腔注射的半数有效剂量(ED50)为0.10毫克/千克。PCP的ED50为腹腔注射0.7毫克/千克。因此,MK-801是一种非常强效的类PCP药物,可能与PCP共享细胞机制和其他效应,包括对NMDA的拮抗作用。

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