The action of six antagonists of the excitatory amino acids on neurones of the rat spinal cord.
The differential susceptibility to blockade by six antagonists of the excitatory actions produced by a number of acidic amino acids has been determined. Four of these, DL-alpha-aminoadipate, 2-amino-5-phosphonovalerate, 2-amino-6-phosphonocaproate and gamma-D-glutamylglycine block the action of N-methyl-D-aspartate (NMDA) most effectively and those of L-glutamate, trans-1-amino-1,3-dicarboxycyclopentane (trans-ADCP) and kainate the least. Cis-2,3-piperidine dicarboxylate resembles the other four, save in that kainate excitations are also powerfully blocked. L-glutamate diethylester was most effective against L-glutamate and least against NMDA: kainate and trans-ADCP excitations were also relatively unaffected. The data support the hypothesis of the existence of at least three classes of amino acid receptor (NMDA-, L-glutamate- and kainate-excited), and the possibility of a fourth category activated by trans-ADCP must be considered.
D000596:Amino Acids / Q000494:pharmacology*; D000818:Animals; D001224:Aspartic Acid / Q000031:analogs & derivatives / Q000494:pharmacology; D005971:Glutamates / Q000494:pharmacology; D018698:Glutamic Acid; D007608:Kainic Acid / Q000494:pharmacology; D016202:N-Methylaspartate; D009474:Neurons / Q000187:drug effects / Q000502:physiology*; D051381:Rats; D013116:Spinal Cord / Q000187:drug effects / Q000502:physiology*; D013329:Structure-Activity Relationship
D000596:Amino Acids; D005971:Glutamates; D001224:Aspartic Acid; D018698:Glutamic Acid; D016202:N-Methylaspartate; D007608:Kainic Acid