Abstract
Antagonists of neuronal excitation induced by dicarboxylic amino acids were tested in genetically spastic rats of the Han-Wistar strain. These animals exhibit an increased muscle tone which can be measured as a spontaneous tonic activity in the electromyogram of the gastrocnemius-soleus muscle. Compounds that block excitation due to N-methyl- d-aspartic acid reduced the spontaneous activity measured in the electromyogram in a dose-related manner. The most potent compounds, 2-amino-7-phosphonoheptanoic and kynurenic acids were effective muscle relaxants when given either intraperitoneally or intracerebroventricularly. 2-Amino-5-phosphonopentanoic acid possessed much weaker muscle relaxant activity, while l-glutamic acid diethylester was inactive by either route. The results suggest that blockade of N-methyl- d-aspartic acid receptors results in a myorelaxant effect. Specific antagonists of excitation at N-methyl- d-aspartic acid receptors may provide a new class of muscle relaxants.
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