Comparative effects of etomidate and its fluoro analogue, R 8110 on testicular, adrenal and ovarian steroid biosynthesis
| Autor: | C. Haelterman, R. Doolaege, D. Beerens, R. De Coster, N. Goeminne, W. Wouters, M. D. W. G. Krekels |
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| Rok vydání: | 1988 |
| Předmět: |
Male
endocrine system medicine.medical_specialty endocrine system diseases medicine.drug_class Guinea Pigs Alpha (ethology) Biology chemistry.chemical_compound Corticosterone Etomidate Adrenal Cortex Hormones Internal medicine Adrenal Glands medicine Animals Hypnotics and Sedatives Aromatase Gonadal Steroid Hormones Testosterone Cells Cultured Pharmacology Granulosa Cells General Veterinary Cholesterol Leydig Cells Rats Endocrinology chemistry Mineralocorticoid biology.protein Female Glucocorticoid medicine.drug |
| Zdroj: | Journal of veterinary pharmacology and therapeutics. 11(4) |
| ISSN: | 0140-7783 |
| Popis: | The effects, of etomidate and of its fluoro analogue, R 8110, on adrenal, testicular and ovarian steroid biosynthesis were compared using cultures of guinea-pig adrenal, rat adrenal capsular, rat testicular and rat ovarian granulosa cells. At a concentration of 100 nM, etomidate inhibited the adrenal 11-hydroxylation of glucocorticoid and mineralocorticoid biosyntheses, producing a decrease in cortisol and corticosterone and an accumulation of 11-deoxycortisol and 11-deoxycorticosterone in guinea-pig adrenal and rat capsular adrenal cell suspensions, respectively. At higher concentrations (greater than 10(-6) M), etomidate also inhibited ovarian oestradiol production, testicular androgen formation and ovarian progesterone synthesis. The latter action suggests an effect on ovarian aromatase, on testicular 17 alpha/17,20-lyase activities and finally on cholesterol side-chain cleavage. The fluoro analogue of etomidate, R 8110, was ten times less potent as an inhibitor of 11-hydroxylation and affected progesterone formation only slightly in adrenal cell suspensions. Testosterone production was less affected by R 8110 than by etomidate. The increase of progestins suggests that the 17 alpha/17,20-lyase activities are the most sensitive testicular enzymatic reactions to R 8110. For inhibition of ovarian oestradiol production, R 8110 was twenty times more potent than etomidate. |
| Databáze: | OpenAIRE |
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