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Abstract
1. 4-Aminomethylbenzenesulphonamide (homosulphanilamide) labelled with 35S has been synthesized.
2. When the labelled drug was given orally to rats, rabbits, guinea pigs and rhesus monkeys, it was mainly deaminated to 4-carboxybenzenesulphonamide, but to a lesser extent in the rat (about 50% of the 24 h excretion) than in the other three species (about 70–90%).
3. Some unchanged drug and a new metabolite, the N4-acetyl derivative, were also excreted, more in the rat than the other three species.
4. Pretreatment of rat, rabbit and guinea pig with antabuse caused more rapid excretion of 35S but did not alter the proportions of the metabolites.
5. In rats and rabbits about the same amount of 35S and the carboxylic acid was excreted whether the drug was given orally or intravenously, but after intravenous injection a smaller proportion of the drug was acetylated compared with oral administration.
6. Pretreatment of rats and rabbits with the monoamine oxidase inhibitor, iproniazid, caused considerable inhibition of deamination and the drug was mainly excreted unchanged and as its N4-acetyl derivative, although the ratio of unchanged to acetylated drug was not significantly different from that when no inhibitor was used. The route of administration of the inhibitor had no effect on the proportions of the metabolites excreted whether the drug was given orally or intravenously. These results would suggest that the drug was mainly deaminated in the liver and other internal tissues rather than the gut wall.