Denitrosation as a determinant of nitrosocimetidine in vivo activity

• Published in: Cancer research (Chicago, Ill.) Vol. 43; no. 11; pp. 5258 - 5267
• Main Author: JENSEN, D. E
• Format: Journal Article
• Language: English
• Published: Philadelphia, PA American Association for Cancer Research 01.11.1983
• Subjects: Amino Acids - metabolism; Animals; Biological and medical sciences; Carbon Radioisotopes; Carcinogens; Chromatography, High Pressure Liquid; Cimetidine - analogs & derivatives; Cimetidine - metabolism; Cimetidine - toxicity; Dimethylnitrosamine - metabolism; Drug toxicity and drugs side effects treatment; Female; Hemoglobins - metabolism; Kinetics; Medical sciences; Methylnitronitrosoguanidine - metabolism; Miscellaneous (drug allergy, mutagens, teratogens...); Pharmacology. Drug treatments; Rats; Rats, Inbred F344; Nitrosation; Metabolism toxicity relation

The widely used drug cimetidine (Tagamet) can be nitrosated in the presence of nitrite and under mild acid conditions to form a compound, nitrosocimetidine (NC), which has a chemical structure very similar to those of the mutagens and laboratory carcinogens N-methyl-N'-nitro-N-nitrosoguanidine...