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The effect of 450191-S, one of the 1H-1,2,4-triazolyl benzophenone derivatives and possessing benzodiazepine-like anti-anxiety actions, on the content of various amino acids in the mouse brain was examined in comparison with that of nitrazepam. Among the various amino acids examined, only glycine, aspartic acid and alanine showed a statistically significant decrease following the oral administration of 450191-S. The oral administration of nitrazepam also induced a similar decline in the cerebral contents of glycine and alanine. Furthermore, it was found that the administration of Ro 15-1788, a benzodiazepine antagonist, eliminated the 450191-S-induced decline in the cerebral contents of glycine and aspartic acid. These results indicate that the administration of 450191-S induces the decrease of glycine and aspartic acid, neuroactive amino acids, in the brain, possibly via the activation of benzodiazepine receptors.

Effect of 450191-S, a 1H-1,2,4-Triazolyl Benzophenone Derivative, on Cerebral Content of Neuroactive Amino Acids