Hashiguchi M, Ebihara A
Department of Clinical Pharmacology and Therapeutics, Oita Medical University, Japan.
Clin Pharmacol Ther. 1992 Sep;52(3):274-6. doi: 10.1038/clpt.1992.141.
The frequency distribution of N-acetylation of caffeine was determined in 140 unrelated healthy Japanese subjects by measuring the amount of two main metabolites of caffeine, 5-acetylamino-6-formyl-amino-3-methyluracil (AFMU) and 1-methylxanthine (1X), in urine after an oral dose of caffeine. N-Acetylation capacity for caffeine appeared to be polymorphic: 15 subjects (10.7%) were phenotyped as slow acetylators, whereas 125 subjects (89.3%) were phenotyped as rapid ones. The urinary molar excretion ratio of AFMU (AFMU/1X) in 2 hours-urine samples ranged from 0.03 (slow acetylators) to 2.66 (rapid acetylators). The frequency of slow acetylators in this study was similar to that reported previously for the isoniazid and dapsone polymorphism in Japanese populations.
通过测量口服咖啡因后尿液中咖啡因的两种主要代谢产物5-乙酰氨基-6-甲酰氨基-3-甲基尿嘧啶（AFMU）和1-甲基黄嘌呤（1X）的量，在140名无亲缘关系的健康日本受试者中确定了咖啡因N-乙酰化的频率分布。咖啡因的N-乙酰化能力似乎具有多态性：15名受试者（10.7%）表现为慢乙酰化者，而125名受试者（89.3%）表现为快乙酰化者。2小时尿液样本中AFMU的尿摩尔排泄率（AFMU/1X）范围为0.03（慢乙酰化者）至2.66（快乙酰化者）。本研究中慢乙酰化者的频率与先前报道的日本人群中异烟肼和氨苯砜多态性的频率相似。
