Garattini S
Acta Psychiatr Scand Suppl. 1978(274):9-18. doi: 10.1111/j.1600-0447.1978.tb02382.x.
Oxazepam is the final metabolic product in vitro and in vivo of a large number of pharmacologically active benzodiazepines. Oxazepam shows antimetrazol activity varying in intensity and duration according to the animal species considered. This difference is in part related to different "sensitivity" and in part due to different disposition of oxazepam. Particularly relevant is the difference in biliary excretion by various animal species. Oxazepam is currently available as a racemate but two optical isomers can be separated as succinate half esters. The (+) form appears to be more active than the (-) form, probably because more oxazepam is released from the (+) than the (-) isomer in vivo. In vitro studies confirm that the liver hydrolyzes the (+) oxazepam succinate half ester more than the (-) form. Other work has aimed at analyzing the effects of oxazepam on brain chemical mediators, with particular reference to the cholinergic system. Finally it is shown that oxazepam, similarly to other benzodiazepines, increased aggressiveness in male mice during chronic treatment.
奥沙西泮是多种具有药理活性的苯二氮䓬类药物在体外和体内的最终代谢产物。奥沙西泮表现出抗戊四氮活性，其强度和持续时间因所研究的动物物种而异。这种差异部分与不同的“敏感性”有关，部分是由于奥沙西泮的不同处置方式。特别相关的是不同动物物种胆汁排泄的差异。奥沙西泮目前以消旋体形式存在，但两种光学异构体可以作为琥珀酸半酯分离出来。（+）形式似乎比（-）形式更具活性，这可能是因为体内从（+）异构体释放的奥沙西泮比（-）异构体更多。体外研究证实，肝脏对（+）奥沙西泮琥珀酸半酯的水解作用比对（-）形式更强。其他研究旨在分析奥沙西泮对脑化学介质的影响，特别是针对胆碱能系统。最后表明，与其他苯二氮䓬类药物类似，奥沙西泮在慢性治疗期间会增加雄性小鼠的攻击性。
