Some Activities of a Potent Steroidal Antiestrogen

Bialy, G.; Merrill, Anne P.; Pincus, Gregory

doi:10.1210/endo-79-1-125

Cited by 11 publications

(2 citation statements)

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“…It produced a moderate lowering of pituitary and serum levels of LH and FSH, and pituitary enlargement, and markedly depressed the weights of the androgen-dependent target organs : the testis, epididymis, seminal vesicles and prostate. This compound is an exceptionally potent anti-oestrogen (Bialy, Merrill & Pincus, 1966), but, unlike other available steroidal and non-steroidal anti-oestrogens, has no inherent oestrogenic activity as reflected by the fact that it eliminates cornified cells in the vaginae of intact female rats for up to 2 weeks after a single injection (B. H. Shapiro, unpublished observation). 19-Norspiroxenone is not anti-androgenic, and although a potent progestin in the immature rabbit, it is only weakly uterotrophic in the mouse (Bialy et al 1966).…”

Section: Enzyme Inhibition In Vivomentioning

confidence: 99%

“…This compound is an exceptionally potent anti-oestrogen (Bialy, Merrill & Pincus, 1966), but, unlike other available steroidal and non-steroidal anti-oestrogens, has no inherent oestrogenic activity as reflected by the fact that it eliminates cornified cells in the vaginae of intact female rats for up to 2 weeks after a single injection (B. H. Shapiro, unpublished observation). 19-Norspiroxenone is not anti-androgenic, and although a potent progestin in the immature rabbit, it is only weakly uterotrophic in the mouse (Bialy et al 1966). We have found (unpublished) that it is anti-uterotrophic in rats, since the uterine weight in adult female Sprague-Dawley rats, treated with daily s.c. doses of 10 mg/kg in DMSO for 24 days, was reduced from 153-6 ±22-5 (s.d.)…”

Section: Enzyme Inhibition In Vivomentioning

confidence: 99%

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Effects of New Multi-Site Hormone Blockers on the Fertility of Male Rats

Goldman¹,

Bh²,

Aw³

1976

Journal of Endocrinology

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The effects on the fertility of adult male rats of six new synthetic steroids: I, 3-cyano-5alpha-androst-1-en-17-one; II, the 17beta-acetate form of I; III, 17beta-hydroxy-5beta-cyano-androstan-3-one; IV, 6-methylpregnenolone; V, 17beta-hydroxy-17alpha-ethynyl-5beta-cyano-19-norandrostan-3-one; and VI, 19-norspiroxenone (oestr-4-en-3-one-spiro-17alpha-2'-[tetrahydrofuran]) have been tested. After 6 weeks of treatment with daily doses of 5 mg (I, II, III), 15 mg (IV) or 10 mg (V, VI) only steroid VI blocked the completion of spermatogenesis and reduced the number of foetuses sired in at least five females/male. Steroid VI also diminished seminal vesicular, prostatic, testicular and epididymal weights. It inhibited the testicular enzymes, 3beta-hydroxysteroid dehydrogenase-delta4-5-3-oxosteroid isomerase system, 17alpha-hydroxylase, and C17-20 lyase markedly, but did not affect the adrenal dehydrogenase-isomerase system. It depressed, strikingly, testicular and serum levels of testosterone and 5alpha-dihydrotestosterone and reduced pituitary and serum levels of FSH and LH. Although marked depression of target organ weights also occurred with steroids II, IV and V, and reduction of androgen levels and LH in the circulation with III, IV and V, only VI was a potent blocker of male fertility with the exception of a slight block of the siring of viable foetuses by steroids IV and V. The major difference in site of action of steroid VI from the others was the depression of pituitary and serum levels of FSH along with a marked diminution of testicular content of both testosterone and 5alpha-dihydrotestosterone. 19-Norspiroxenone in the rat is a potent anti-oestrogen without inherent oestrogenicity and is anti-uterotrophic. Thus, VI may affect male fertility by virtue of its potent anti-oestrogenic action in the hypothalamus or testis.

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Section: Enzyme Inhibition In Vivomentioning

confidence: 99%

Section: Enzyme Inhibition In Vivomentioning

confidence: 99%