Croucher M J, Collins J F, Meldrum B S
Science. 1982 May 21;216(4548):899-901. doi: 10.1126/science.7079744.
Compounds that antagonize neuronal excitation induced by dicarboxylic amino acids were tested in two animal models of epilepsy, namely sound-induced seizures in DBA/2 mice and threshold pentylenetetrazol seizures in Swiss mice. Sound-induced seizures could be prevented by intracerebroventricular injection of compounds that block excitation due to N-methyl-D-aspartic acid. The most potent such compound, 2-amino-7-phosphonoheptanoic acid, was anticonvulsant in both test systems when given either intraperitoneally or intracerebroventricularly. Specific antagonists of excitation that is caused by amino acids provide a new class of anticonvulsant agents.
在两种癫痫动物模型中测试了拮抗二羧酸氨基酸诱导的神经元兴奋的化合物,即DBA/2小鼠的声音诱导性癫痫发作和瑞士小鼠的阈下戊四氮癫痫发作。脑室内注射阻断N-甲基-D-天冬氨酸引起的兴奋的化合物可预防声音诱导性癫痫发作。最有效的此类化合物2-氨基-7-膦酰庚酸,腹腔内或脑室内给药时在两种测试系统中均具有抗惊厥作用。由氨基酸引起的兴奋的特异性拮抗剂提供了一类新的抗惊厥药物。