Metabolism of tiaramide in vitro III. Sulphoconjugation of alicyclic amine and alcoholic hydroxyl group by hepatic 105 000 g supernatants

Abstract

1. Sulphoconjugation of the alicyclic secondary amine, DETR (the N-dealkylated metabolite of tiaramide) and of the alcoholic hydroxyl group of tiaramide were observed in liver 105 000 g supernatants of rats and mice but hardly detected in hepatic microsomes.

2. The activities depended on active sulphate, 3′-phosphoadenosine 5′-phosphoa-sulphate, or its generating system.

3. Sulphoconjugation of DETR and tiaramide by the supernatants of female rats and mice proceeded more rapidly than those of males, and sex differences were observed irrespective of sulphate donors, the active sulphate or its generating system.

4. Sulphoconjugation of the alicyclic amine and of the alcohol exhibited different pH optima and different susceptibilities to salts.