Soine W H, Soine P J, England T M, Ferkany J W, Agriesti B E
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond 23298-0581.
J Pharm Sci. 1991 Feb;80(2):99-103. doi: 10.1002/jps.2600800202.
Previously, the N-glucosylation of phenobarbital had been observed only in humans. The results of a species screen (mouse, rat, guinea pig, rabbit, cat, dog, pig, and monkey) found that only mice excreted the N-glucosides of phenobarbital in urine after ip administration of sodium phenobarbital. The major diastereomer excreted by the mouse had the R configuration at the C-5 position of the barbiturate ring. The N-glucoside metabolites accounted for a small percentage of the dose (approximately 0.5%). Following ip dosing of the mouse with the phenobarbital N-glucosides, free phenobarbital could be detected in the urine. Upon ip or intercerebroventricular (icv) injection of the phenobarbital N-glucosides, minimal CNS activity was observed in the mouse.
此前，仅在人类中观察到苯巴比妥的N-糖基化现象。一项物种筛选（小鼠、大鼠、豚鼠、兔子、猫、狗、猪和猴子）结果发现，腹腔注射苯巴比妥钠后，只有小鼠在尿液中排泄出苯巴比妥的N-糖苷。小鼠排泄的主要非对映异构体在巴比妥环的C-5位具有R构型。N-葡糖苷代谢物占给药剂量的比例较小（约0.5%）。给小鼠腹腔注射苯巴比妥N-糖苷后，尿液中可检测到游离苯巴比妥。腹腔注射或脑室内注射苯巴比妥N-糖苷后，在小鼠中观察到的中枢神经系统活性极小。
