Batten P L, Hathway D E
Br J Cancer. 1977 Mar;35(3):342-6. doi: 10.1038/bjc.1977.48.
N-Dephenylation of N-phenyl-2-naphthylamine (PBNA) is strictly limited in dogs, and a 5 mg/kg dose gives 0-10 microng of urinary 2-naphthylamine (BNA), which does not appear to undergo further metabolism. Neither 2-naphthylhydroxylamine (BNHA) nor 2-amino-1-naphthylsulphate were detected in the urine of treated animals. Urinary output of BNA varies markedly between dogs, and at different times in the same animal. The extent of PBNA N-dephenylation is unaltered by chronic administration. Calculations based on Druckery and Küpfmüller's equation (1948) and present data indicate that, for dogs to form BNA tumours through exposure to a relatively high dose-level of PBNA, the period of daily dosing would occupy, or even exceed, the normal life-span. The carcinogenic risk of PBNA to human subjects is discussed.
N-苯基-2-萘胺（PBNA）的N-去苯基化在犬类中受到严格限制，5毫克/千克的剂量会产生0至10微克的尿2-萘胺（BNA），且其似乎不会进一步代谢。在接受治疗的动物尿液中未检测到2-萘基羟胺（BNHA）和2-氨基-1-萘基硫酸盐。BNA的尿量在不同犬类之间以及同一动物的不同时间存在显著差异。长期给药不会改变PBNA的N-去苯基化程度。基于德鲁克里（Druckery）和屈普夫米勒（Küpfmüller）方程（1948年）及现有数据的计算表明，对于犬类通过暴露于相对高剂量水平的PBNA形成BNA肿瘤而言，每日给药的时长将占据甚至超过正常寿命。文中还讨论了PBNA对人类受试者的致癌风险。
