Muscle relaxant action of excitatory amino acid antagonists |
| |
Authors: | L Turski M Schwarz W A Turski T Klockgether K H Sontag J F Collins |
| |
Institution: | 1. Department of Pharmacology and Therapeutics, Faculty of Medicine, The University of British Columbia, Vancouver, B.C., V6T 1W5 Canada;2. Clarke Institute of Psychiatry, Toronto, Ont., M5T 1R8 Canada |
| |
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. |
| |
Keywords: | N-methyl-4-phenyl-1 2 3 6-tetrahydropyridine MPTP N-methyl-4-phenylpyridinium ion dopamine striatum substantia nigra neurotoxicity Parkinson's disease mouse |
本文献已被 ScienceDirect 等数据库收录! |