Maksay G, Kardos J, Simonyi M, Tegyey Z, Otvös L
Arzneimittelforschung. 1981;31(6):979-81.
Six aliphatic esters of oxazepam were investigated for 3H-diazepam displacing activity and hydrolysis in rat in the brain P2-fraction treated with diisopropylfluorophosphate. The esters are prodrugs in relation to oxazepam. Increasing size of the 3-substituent and steric hindrance increased the value of IC50. Controversial reports on oxazepam hemisuccinate could be explained by its stereoselective hydrolysis in vivo.
研究了6种奥沙西泮的脂肪族酯在经二异丙基氟磷酸处理的大鼠脑P2组分中的3H-地西泮取代活性及水解情况。这些酯相对于奥沙西泮而言是前体药物。3-取代基尺寸的增加和空间位阻提高了IC50值。关于奥沙西泮半琥珀酸酯的争议性报道可以通过其在体内的立体选择性水解来解释。
