Kammerer R C, Froines J R, Price T
Food Chem Toxicol. 1986 Sep;24(9):981-5. doi: 10.1016/0278-6915(86)90327-3.
Methapyrilene, four structurally related antihistamines, three metabolites of methapyrilene and two products of the reaction of methapyrilene with nitrite were all tested for mutagenicity to Salmonella typhimurium. The two products of the methapyrilene-nitrite reaction have also been identified as metabolites of methapyrilene. None was mutagenic alone, either with or without rat liver S-9 activation. After reaction with sodium nitrite in acetic acid solution (nitrosation), the products of five of the ten compounds were mutagenic. These compounds were methaphenilene, 2-thiophenemethanol, 2-thiophenecarboxylic acid, N-(2-pyridyl)-N'N'-dimethylethylenediamine and N-(2-thenylmethyl)-2-aminopyridine.
对甲哌啶、四种结构相关的抗组胺药、甲哌啶的三种代谢产物以及甲哌啶与亚硝酸盐反应的两种产物，均进行了对鼠伤寒沙门氏菌的致突变性测试。甲哌啶 - 亚硝酸盐反应的两种产物也已被鉴定为甲哌啶的代谢产物。单独使用时，无论有无大鼠肝脏S - 9活化，这些物质均无致突变性。在乙酸溶液中与亚硝酸钠反应（亚硝化）后，十种化合物中的五种产物具有致突变性。这些化合物是甲苯哌啶、2 - 噻吩甲醇、2 - 噻吩羧酸、N - (2 - 吡啶基)-N'N'-二甲基乙二胺和N - (2 - 噻吩甲基)-2 - 氨基吡啶。
