RESUMO
1. Rats exhibit a sex difference in the rate of metabolism of endrin. 2. The major metabolite in both sexes is anti-12-hydroxyendrin which is excreted via the bile as the glucuronide. Male rats produce the metabolite at a higher rate than do females. 3. trans-4,5-Dihydroisodrin-4,5-diol is a minor metabolite. A mechanism for its formation is discussed. 4. There is a sex difference in the production and excretion of 12-ketoendrin which is observed as a urinary metabolite in male rat; the major urinary metabolite in female rats is anti-12-hydroxyendrin O-sulphate. 5. syn-12-Hydroxyendrin was not detected but may be an intermediate in the formation of 12-ketoendrin. 6. The formation of 12-ketoendrin is related to the acute toxicity of endrin.
Assuntos
Endrin/metabolismo , Tecido Adiposo/metabolismo , Animais , Bile/metabolismo , Endrin/toxicidade , Endrin/urina , Fezes/análise , Feminino , Glucuronatos/metabolismo , Inativação Metabólica , Rim/metabolismo , Fígado/metabolismo , Masculino , RatosRESUMO
1. [14C]Endrin, administered orally to rabbits, is excreted in the faeces as unchanged endrin (50% of that administered) and in the urine as a mixture of polar metabolites. 2. The major biotransformation is hydroxylation at the methylene bridge (C-12) to yield anti-12-hydroxyendrin. syn-Hydroxylation at C-12 also occurs. 3. The hydroxylated metabolites are excreted mainly as their sulphate conjugates. 4. Glucuronide conjugates are also excreted. anti-12-Hydroxyendrin is rapidly conjugated in vitro on incubation with rabbit liver microsomal glucuronyl transferase and UDPGA. 5. Comparative aspects of the metabolism of endrin in rats and rabbits are discussed.