Danazol inhibits steroidogenesis in the rat testis in vitro
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⤵ 26 in-corpus citations
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Danazol suppressed LH-stimulated testosterone and androstenedione production in rat Leydig cells and directly inhibited multiple microsomal enzymes involved in testicular steroidogenesis <i>in vitro</i>.
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Abstract
The effects of danazol on steroidogenesis in vitro in the rat testis were examined by studying: 1) androgen synthesis in rat Leydig cells cultured with danazol, 2) danazol binding to rat testis microsomal cytochrome P-450, and 3) enzyme kinetics of danazol inhibition of the microsomal enzymes of testicular steroidogenesis. Concentrations of danazol as low as 1 micrometer suppressed LH-stimulated testosterone and androstenedione production in cultured Leydig cells. The addition of danazol to a preparation of testicular microsomes elicited a type I cytochrome P-450 binding spectrum, with an apparent spectral dissociation constant (Ks) of 4.8 micrometer. Danazol inhibited progesterone and 17alpha-hydroxy-progesterone binding to microsomal P-450 with apparent spectral inhibition constants of 2.4 micrometer and 2.8 micrometer, respectively. Danazol competitively inhibited 3beta-hydroxy-delta5-steroid dehydrogenase-isomerase (apparent enzymatic inhibition constant, KI = 5.8 micrometer), 17alpha-hydroxylase (KI = 2.4 micrometer), 17,20 lyase (KI = 1.9 micrometer), and 17beta-hydroxysteroid dehydrogenase (KI = 4.4 micrometer). These findings indicate that low concentrations of danazol directly inhibit steroidogenesis in the rat testis in vitro.
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References (8)
- A competitive radioligand assay for danazol (17 alpha-pregn-4-en-20-yno(2,3-d)isoxazol-17-ol) using pregnant guinea pig plasma via openalex
- Clinical studies with an antigonadotropin-Danazol via openalex
- Contraceptive properties of Danazol. via openalex
- Hormonal changes associated with Danazol therapy via openalex
- The effect of danazol in sexual precocity via openalex
- doi:10.1095/biolreprod10.4.438 via openalex
- doi:10.1016/0006-291x(73)91074-7 via openalex
- doi:10.1007/978-1-4757-0196-8_9 via openalex
Cited by (25)
- Danazol 2022
- Short-term dynamic culture of rat testicular fragments as a model to assess effects on steroidogenesis--potential use and limitations 2009
- A benefit-risk assessment of medical treatment for uterine leiomyomas 2002
- Effects of danazol on endometrial DNA synthesis in rats 1993
- Effects of danazol on DNA synthesis in rat prostate 1993
- Suppression of the development of uterine adenomyosis by danazol treatment in mice 1992
- The use of danazol as a treatment of endometriosis 1991
- Comparison of the pharmacology of nafarelin and danazol 1990
- Effects of danazol on steroidogenesis and gonadotropic responsiveness in isolated human preovulatory follicular cells 1986
- Endocrine effects of danazol in the treatment of endometriosis 1984
- Effect of danazol on gonadal steroidogenesis in patients with a complete form of testicular feminization 1982
- Structural and functional regression of polycystic ovaries by danazol 1981
- Transient adrenogenital syndrome due to exposure to danazol in utero 1981
- Androgen uptake in the female reproductive system of a nonhuman primate 1981
- Actions of danazol in vivo on cytochrome P-450 and steroidogenic enzymes in rat testis and liver microsomal preparations 1981
- Danazol inhibits human adrenal 21-and 11 beta-hydroxylation in vitro 1980
- Danazol suppresses luteal function in vitro and in vivo 1980
- Pharmacology and pharmacokinetics of danazol 1980
- Evidence that danazol inhibits gonadotropin-induced ovarian steroidogenesis at a point distal to gonadotropin-receptor interaction and adenosine 3',5' cyclic monophosphate formation 1980
- Inhibition of adrenal steroidogenesis by danazol in vivo 1980
- Mechanism of induction of luteal phase defects by danazol 1980
- The "treatment" of unexplained infertility with danazol 1979
- Effect of danazol on estradiol-17beta and progesterone secretion by porcine ovarian cells in vitro 1979
- Danazol binding to rat androgen, glucocorticoid, progesterone, and estrogen receptors: correlation with biologic activity 1979
- Increased accumulation of estrogen receptors in pituitary nuclei of danazol treated rats 1979
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- openalex
- last seen: 2026-05-10T10:42:17.238252+00:00
- pubmed
- last seen: 2026-10-08T21:23:18.497579+00:00
- unpaywall
- last seen: 2026-10-16T06:24:35.758740+00:00
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