Zimmer A, Krüger G, Prox A, Stahl E, Wolter B, Wachsmuth H, Köster P
Arzneimittelforschung. 1978;28(4):688-92.
The biotransformation of 3'-chloro-2'-(N-methyl-N-[(morpholino-carbonyl)methyl]aminomethyl)benzanilide hydrochloride (fominoben-HCl, PB 89 Cl, Noleptan) was investigated in man. The most substantial metabolites were quantified. The metabolite patterns of fominoben in urine and plasma are compared. Fominoben, is rapidly and extensively metabolized to many metabolites. At the time of the maximum plasma level. 2 h after an oral dose of 160 mg of 14C-PB 89 Cl, only 1.5% of the plasma radioactivity can be measured as the unchanged initial compound. No parent compound can be found in the urine, only in the stool some traces of fominoben can be detected. The biotransformation can be characterized by four main pathways: 1. cleavage reactions, 2. hydroxylations, 3. cyclisations, 4. conjugations. The reactions 1--3 proceed as well simultaneously as successively.
对盐酸3'-氯-2'-(N-甲基-N-[(吗啉代羰基)甲基]氨甲基)苯甲酰苯胺（福米诺苯盐酸盐，PB 89 Cl，诺来替坦）在人体中的生物转化进行了研究。对最主要的代谢产物进行了定量分析。比较了福米诺苯在尿液和血浆中的代谢产物模式。福米诺苯迅速且广泛地代谢为多种代谢产物。口服160 mg 14C-PB 89 Cl后2小时，即血浆浓度达到峰值时，血浆放射性中仅1.5%可测得为未变化的初始化合物。尿液中未发现母体化合物，仅在粪便中可检测到少量福米诺苯。生物转化可通过四条主要途径来表征：1. 裂解反应；2. 羟基化反应；3. 环化反应；4. 结合反应。反应1至3既可以同时进行，也可以相继进行。
