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Molecular Pharmacology, Vol 14, 940-949, Copyright © 1978 by the American Society for Pharmacology and Experimental Therapeutics

Genetic Variation in N-Acetylation of Carcinogenic Arylamines by Human and Rabbit Liver

IRENE B. GLOWINSKI 1, HAROLD E. RADTKE 1, and WENDELL W. WEBER 1

1 Department of Pharmacology, University of Michigan, Ann Arbor, Michigan 48109

The arylamine carcinogens aminofluorene, agr-naphthylamine, beta-naphthylamine, benzidine and methylene bis-2-chloroaniline are acetylated by the same polymorphic N-acetyltransferase (EC 2.3.1.5) as isoniazid and sulfamethazine in human and rabbit populations. Apparent Km values for these carcinogens determined with human and rabbit N-acetyl-transferases obtained from rapid and slow isoniazid acetylator individuals are approximately one order of magnitude smaller than for the polymorphic drug substrate, sulfamethazine. The apparent Km values for all the carcinogens and sulfamethazine were also strongly correlated with their octanol-water partition coefficients indicating that their kinetic properties are highly dependent upon their hydrophobic nature. Since differences in susceptibility to toxicity from isoniazid, hydralazine and procainamide are associated with different acetylator phenotypes, the possibility is raised that rapid and slow isoniazid acetylator populations may differ in susceptibility to chemical carcinogenicity from exposure to arylamines.

Submitted on January 30, 1978
Accepted on April 17, 1978




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Y.W. F. Lam and M. V. Marshall
Genetically Determined Polymorphisms in Drug Metabolism
Journal of Pharmacy Practice, January 1, 1992; 5(6): 317 - 336.
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