Indoxyl derivatives of drug metabolites

Summary Indoxyl derivatives were detected as minor products among the urinary metabolites of two trial drugs, a benzodiazepine (GP 55 129) and a benzophenone (CGP 11 952). Their structures were elucidated by NMR and mass spectroscopy. Presumably, metabolites containing potential aldehyde functions react spontaneously with endogenous indoxyl. Such derivatives have not hitherto been encountered in drug metabolism.     

Single injections of triazolam,a short-acting benzodiazepine,lengthen the period of the circadian activity rhythm in golden hamsters

Single injections of the benzodiazepine, triazolam, induce phase shifts and cause a lengthening of the circadian activity rhythm in the golden hamster. The effect of triazolam on period depends on the phase of injection, but is not dependent on the direction of the phase shifts. Triazolam injections caused increases in period that were associated with phase advances as well as phase delays in the activity rhythm. This relationship between triazolam-induced phase shifts and changes in period is different from the relationship between light-induced phase shifts and period changes.     

苯二氮■化合物等对雌性狼山鸡生产性能的影响

本试验研究苯二氮化合物－Ｆ８９以及β－受体激动剂ｃｌｅｎｂｕｔｅｒｏｌ（ＣＬ）对雌性狼山鸡生产性能的影响。２ｐｐｍＦ８９和２ｐｐｍＦ８９＋１ｐｐｍＣＬ添加在６５－１１５日龄雌性狼山鸡日粮中，能分别提高摄食量１１．３９％和７．５８％，提高增重２０．４６％（ｐ＜０．０１）和１５．３３％（ｐ＜０．０５）；降低料重比７．５２％和６．７１％。屠宰测定表明：日粮中添加２ｐｐｍＦ８９对狼山鸡胴体组成没有影响．而添加２ｐｐｍＦ８９＋１ｐｐｍｃＬ却提高了鸡的胸肌率１１．２８％（ｐ＜０．０１）、腿肌率６．７７％（ｐ＜０．０５），从而改善动物胴体组成，提高瘦肉率。添喂含２ｐｐｍＦ８９的日粮后，狼山鸡血糖浓度显著下降，β－脂蛋白含量显著上升。表明Ｆ８９影响鸡的糖代谢脂代谢活动。     

反相高效液相色谱法测定7种苯二氮(艹卓)类药物的研究

用反相梯度高效液相色谱法研究并同时测定了7种苯二氮革类药物（Benzodiazepines，BZDs），并将该方法应用于血清和尿液中的BZDs类药物测定．在本实验条件下，测定血清和尿液样品，方法精密度（RSD）不大于10％，回收率在94％～110％间，在较宽的范围内峰面积与浓度呈良好的线性关系，相关系数均在0．9992以上．地西泮、硝西泮、艾司唑仑、阿普唑仑的检出限分别为2ng·mL^-1，7ng·mL^-1，5．5ng·mL^-1及6ng·mL^-1；而氯硝西泮、三唑仑和咪达唑仑的检出限均为5ng·mL^-1．将本法用于分析体内BZDs，可以在40min内分离测定7种BZDs，方法操作简便、结果准确可靠，适于血清及尿液等生物样品中这类药物含量的测定．