Pfeifer S, Gedan A, Franke P, Klemm W, Morgenroth U
Sektion Chemie, Humboldt-Universität zu Berlin.
Pharmazie. 1990 Jul;45(8):603-7.
After p.o. administration to rats AWD 26-06 (1) is rapidly but incompletely absorbed. The relatively short distribution (t1/2 alpha = 37 min) is followed by a middle-long elimination (t1/2 beta = 14 h). The volumen of distribution do not suggest an uncommon accumulation in deep compartments. About 70% of 1 were excreted unchanged with the feces. In urine and feces 18 metabolites were identified. The structure of 10 products could be elucidated. All metabolites have changed side-chains. Furthermore, the tricyclic molecule without side-chain and a N-methyl derivative were identified. The metabolites with so far unknown structure contain the unsubstituted tricyclic moiety too.
大鼠口服给药后,AWD 26 - 06 (1)吸收迅速但不完全。分布相对较短(t1/2α = 37分钟),随后是中长程消除(t1/2β = 14小时)。分布容积表明在深部隔室中没有异常蓄积。约70%的1以原形随粪便排出。在尿液和粪便中鉴定出18种代谢产物。其中10种产物的结构得以阐明。所有代谢产物的侧链均发生了变化。此外,还鉴定出了无侧链的三环分子和一种N - 甲基衍生物。结构迄今未知的代谢产物也含有未取代的三环部分。