3-(2,6-二甲基苯基)-5-甲基乙内酰脲——大鼠体内妥卡尼的一种代谢物或代谢产物。

3-(2,6-Xylyl)-5-methylhydantoin--a metabolite or a metabonate of tocainide in rats.

Venkataramanan R, Axelson J E

Xenobiotica. 1981 Apr;11(4):259-65. doi: 10.3109/00498258109045300.

Abstract

G.1.c.-mass spectrometric analysis of urine extracts from rats dosed with tocainide (I) revealed the presence of cyclic compound identified as 3-(2,6-xylyl)-5-methylhydantoin (IV) derived from tocainide. 2. Evidence indicates that IV is derived from a conjugate of tocainide (tocainide carbonyl O-beta-D-glucuronide) (III) in humans. 3. Results of the present study indicate that in addition to being formed from a conjugate, IV is generated directly from tocainide in vivo in rats. Possible mechanisms for the formation of IV in rats in vivo are discussed.

摘要

G.1.c. 对用妥卡尼（I）给药的大鼠尿液提取物进行质谱分析，结果显示存在一种环状化合物，鉴定为源自妥卡尼的3-(2,6-二甲苯基)-5-甲基乙内酰脲（IV）。2. 有证据表明，在人体内，IV源自妥卡尼的一种结合物（妥卡尼羰基O-β-D-葡萄糖醛酸苷）（III）。3. 本研究结果表明，除了由结合物形成外，IV在大鼠体内还直接由妥卡尼生成。讨论了IV在大鼠体内形成的可能机制。