竞争性N-甲基-D-天冬氨酸受体拮抗剂CGP 40116可替代乙醇的辨别性刺激效应。
Competitive NMDA receptor antagonist, CGP 40116, substitutes for the discriminative stimulus effects of ethanol.
作者信息
Bienkowski P, Stefanski R, Kostowski W
机构信息
Department of Pharmacology and Physiology of the Nervous System, Institute of Psychiatry and Neurology, Warsaw, Poland.
出版信息
Eur J Pharmacol. 1996 Oct 31;314(3):277-80. doi: 10.1016/s0014-2999(96)00658-9.
A drug discrimination procedure was used to compare the ability of competitive (CGP 37849, D,L-(E)-2-amino-4-methyl-5-phosphono-3-pentanoate; CGP 40116, D-(E)-2-amino-4-methyl-5-phosphono-3-pentanoate) and non-competitive (dizocilpine) NMDA receptor antagonists to substitute for ethanol in rats trained to discriminate between a 1.0 g/kg dose of ethanol (i.p.) and saline. Dizocilpine (0.1-0.3 mg/kg) substituted partially for ethanol at doses that markedly reduced the rate of responding. CGP 37849 (1.25-5.0 mg/kg) substituted partially for ethanol and suppressed the response rate. CGP 40116 (0.5-2.5 mg/kg), and active D-stereoisomer of CGP 37849, completely substituted (88%) for ethanol, and caused only moderate suppression of the response rate.
采用药物辨别程序，比较竞争性NMDA受体拮抗剂（CGP 37849，D，L-（E）-2-氨基-4-甲基-5-膦酰基-3-戊酸酯；CGP 40116，D-（E）-2-氨基-4-甲基-5-膦酰基-3-戊酸酯）和非竞争性NMDA受体拮抗剂（地佐环平）替代乙醇的能力，这些大鼠已被训练区分1.0 g/kg剂量的乙醇（腹腔注射）和生理盐水。地佐环平（0.1 - 0.3 mg/kg）在显著降低反应率的剂量下部分替代乙醇。CGP 37849（1.25 - 5.0 mg/kg）部分替代乙醇并抑制反应率。CGP 40116（0.5 - 2.5 mg/kg），即CGP 37849的活性D-立体异构体，完全替代（88%）乙醇，且仅适度抑制反应率。
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