（3H）苯甲酰去甲可卡因（可卡因代谢物）在大鼠体内的处置情况。

Disposition of (3H) benzoylnorecgonine (cocaine metabolite) in the rat.

作者信息

Misra A L, Giri V V, Patel M N, Alluri V R, Pontani R B, Mule S J

出版信息

Res Commun Chem Pathol Pharmacol. 1976 Apr;13(4):579-84.

Abstract

The preparation and disposition of (3H) benzoylnorecgonine, which has potent stimulant activity intracisternally in the rat, has been described. The T1/2 of (3H) benzoylnorecgonine in brain and plasma of rats injected with a 10 mg kg-1 i.v. dose were 3.0, 1.2 h respectively. The ratio of mean peak concentration in brain to that in plasma was 0.03. No metabolites of benzoylnorecgonine were observed in rat brain. The mean percentage of dose excreted in urine and feces in 96 h were 85 and 2.2, respectively, with major excretion (82.5%) occurring within 24 h in urine. Approximately 90% of the radioactivity in urine was due to unmetabolised benzoylnorecgonine and 10% due to an unidentified metabolite. Norecgonine was not detected as a urinary metabolite.

摘要

已描述了具有强效刺激活性的（3H）苯甲酰去甲伪麻黄碱在大鼠脑池内的制备和处置情况。给大鼠静脉注射10mg/kg剂量后，（3H）苯甲酰去甲伪麻黄碱在大鼠脑和血浆中的半衰期分别为3.0小时和1.2小时。脑内平均峰值浓度与血浆中平均峰值浓度之比为0.03。在大鼠脑中未观察到苯甲酰去甲伪麻黄碱的代谢产物。96小时内尿液和粪便中排出的剂量平均百分比分别为85%和2.2%，主要排泄（82.5%）在24小时内通过尿液排出。尿液中约90%的放射性是由于未代谢的苯甲酰去甲伪麻黄碱，10%是由于一种未鉴定的代谢产物。未检测到去甲伪麻黄碱作为尿液代谢产物。