Competitive NMDA receptor antagonist, CGP 40116, substitutes for the discriminative stimulus effects of ethanol.
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.
Bienkowski
P
P
Department of Pharmacology and Physiology of the Nervous System, Institute of Psychiatry and Neurology, Warsaw, Poland.
Stefanski
R
R
Kostowski
W
W
D015763:2-Amino-5-phosphonovalerate / Q000031:analogs & derivatives* / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive; D004193:Discrimination Learning / Q000187:drug effects*; D016291:Dizocilpine Maleate / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D000431:Ethanol / Q000494:pharmacology*; D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology*; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism
D018691:Excitatory Amino Acid Antagonists; D016194:Receptors, N-Methyl-D-Aspartate; C064539:2-amino-4-methyl-5-phosphono-3-pentenoic acid; D000431:Ethanol; D016291:Dizocilpine Maleate; D015763:2-Amino-5-phosphonovalerate