AMPA受体拮抗剂GYKI 52466可逆转竞争性NMDA受体拮抗剂CGP 37849的抗僵住效应。

The AMPA receptor antagonist GYKI 52466 reverses the anti-cataleptic effects of the competitive NMDA receptor antagonist CGP 37849.

作者信息

Hauber W, Waldenmeier M T

机构信息

Department of Animal Physiology, Biological Institute, University of Stuttgart, Germany.

出版信息

Eur J Pharmacol. 1994 May 2;256(3):339-42. doi: 10.1016/0014-2999(94)90561-4.

DOI:10.1016/0014-2999(94)90561-4

PMID:7913894

Abstract

The effects of the AMPA receptor antagonist GYKI 52466 (1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine HCl) on haloperidol-induced catalepsy were tested in drug-naive rats and in rats pretreated with the competitive NMDA receptor antagonist CGP 37849 (DL-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid). CGP 37849 (4 mg/kg i.p.) given alone significantly reversed haloperidol-induced catalepsy (0.5 mg/kg i.p.) while GYKI 52466 (4.8 mg/kg i.p.) given alone was without effect. Administration of GYKI 52466 to rats pretreated with CGP 37849 abolished the anticataleptic effects of the competitive NMDA receptor antagonist seen following single administration. Thus the AMPA receptor antagonist prevents behavioural effects induced by a NMDA receptor antagonist in this behavioural model.

摘要

在未用药的大鼠以及预先用竞争性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂CGP 37849（DL-(E)-2-氨基-4-甲基-5-膦酰基-3-戊烯酸）处理过的大鼠中，测试了AMPA受体拮抗剂GYKI 52466（1-(4-氨基苯基)-4-甲基-7,8-亚甲基二氧基-5H-2,3-苯并二氮杂䓬盐酸盐）对氟哌啶醇诱导的僵住症的影响。单独给予CGP 37849（腹腔注射4mg/kg）可显著逆转氟哌啶醇（腹腔注射0.5mg/kg）诱导的僵住症，而单独给予GYKI 52466（腹腔注射4.8mg/kg）则无作用。对预先用CGP 37849处理过的大鼠给予GYKI 52466，消除了单次给药后可见的竞争性NMDA受体拮抗剂的抗僵住症作用。因此，在该行为模型中，AMPA受体拮抗剂可阻止NMDA受体拮抗剂诱导的行为效应。