Bagolini C, de Witt P, Pacifici L, Ramacci M T
J Med Chem. 1978 May;21(5):476-80. doi: 10.1021/jm00203a015.
4-N-Alkylamino derivatives and corresponding ammonium quaternary salts of tetrahydro-1,4-benzodiazepin-5-one were synthesized and evaluated for psychotropic activity in mice by ip via. This study was also extended to some nitro and amino derivatives of tetrahydro-1,4-benzodiazepin-5-one. Compounds were devoid of tranquilizing activity and in comparison with two classical benzodiazepines, chlordiazepoxide and diazepam, they showed high toxicity and little or no effect on motor coordination, motor activity, and maximal electroshock. On some "in vitro" tests the compounds exhibited pharmacological properties when they were used at high concentrations.
合成了四氢-1,4-苯并二氮杂卓-5-酮的4-N-烷基氨基衍生物及其相应的季铵盐，并通过腹腔注射途径在小鼠中评估其精神活性。该研究还扩展到四氢-1,4-苯并二氮杂卓-5-酮的一些硝基和氨基衍生物。这些化合物没有镇静活性，与两种经典苯二氮卓类药物氯氮卓和地西泮相比，它们显示出高毒性，对运动协调、运动活性和最大电休克几乎没有影响。在一些“体外”试验中，这些化合物在高浓度使用时表现出药理特性。
