The effect of the dioxolanes on amino acid induced excitation in the mammalian spinal cord

• Published in: Brain research Vol. 307; no. 1-2; p. 85
• Main Authors: Berry, S C, Anis, N A, Lodge, D
• Format: Journal Article
• Language: English
• Published: Netherlands 30.07.1984
• Subjects: Animals; Aspartic Acid - analogs & derivatives; Aspartic Acid - antagonists & inhibitors; Cats; Dioxolanes - pharmacology; Dioxoles - pharmacology; Kainic Acid - antagonists & inhibitors; Ketamine - pharmacology; N-Methylaspartate; Oxadiazoles - antagonists & inhibitors; Phencyclidine - pharmacology; Quisqualic Acid; Rats; Species Specificity; Spinal Cord - drug effects; Stereoisomerism; Structure-Activity Relationship
• ISSN: 0006-8993
• DOI: 10.1016/0006-8993(84)90463-3

The effects of the dissociative anaesthetic, etoxadrol, and the stereoisomers of dioxadrol, dexoxadrol and levoxadrol, were examined on the excitation of spinal neurones by electrophoretically administered amino acids in pentobarbitone- or urethane-anaesthetized rats, or pentobarbitone-anaesthetized cats. Both etoxadrol and the (+)isomer of dioxadrol, dexoxadrol, administered locally or systemically, exhibited a selective antagonism of N-methyl-D,L-aspartate relative to quisqualate and kainate. This selective antagonism was not observed with the (-)isomer of dioxadrol, levoxadrol. Since such a stereoselective antagonism of the excitation of spinal neurones by N-methyl-D,L-aspartate is also displayed by the dissociative anaesthetics phencyclidine and ketamine, it is suggested that a reduced efficiency at excitatory synapses utilising N-methyl-D,L-aspartate receptors contributes to that part of the pharmacological spectrum common to both arylcyclohexylamines and dioxolanes.