异丙嗪的体外代谢。N-氧化产物的鉴定。

Metabolism of promethazine in vitro. Identificaton of N-oxidized products.

Clement B, Beckett A H

Xenobiotica. 1981 Sep;11(9):609-18. doi: 10.3109/00498258109045872.

Abstract

Incubation of promethazine (Ia) and desmethylpromethazine (Ib) with 9000g supernatant fractions of rabbit liver homogenate resulted in formation of N-dealkylated, N-oxygenated and ring-hydroxylated products. 2. The N-oxidation products identified by t.l.c. and mass spectra using synthetic reference products are promethazine-N-oxide (IX) and the nitrone (VIII), which is believed to be formed chemically and metabolically from the metabolite N-hydroxydesmethylpromethazine (VII).

摘要

将异丙嗪（Ia）和去甲异丙嗪（Ib）与兔肝匀浆9000g上清液组分一起温育，导致形成N-去烷基化、N-氧化和环羟基化产物。2. 通过薄层层析（t.l.c.）和使用合成参考产物的质谱鉴定出的N-氧化产物是异丙嗪-N-氧化物（IX）和硝酮（VIII），据信后者是由代谢物N-羟基去甲异丙嗪（VII）通过化学和代谢方式形成的。