Biological Activities of Some 6-Methylated Progesterones.

Elton, Richard L.; Edgren, Richard A.; Calhoun, David W.

doi:10.3181/00379727-103-25449

Cited by 22 publications

(5 citation statements)

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“…The finding of small adrenals in the megestrol treated rats excluded the possibility that this action is mediated via an increased production of adrenal steroids. Adrenal involution after megestrol acetate administration has previously been demonstrated in female rats (Elton et al 1960;Arenas 1963) but not in intact male rats at dose levels comparable to those given to castrated rats in the present investigation (David et al 1963; Karkun 8c Kar 1965). Arenas (1963) claimed that the adrenal depressant activity of megestrol acetate demonstrated in female rats is due to a direct action on the adrenal glands.…”

Section: Discussionsupporting

confidence: 47%

Androgenic Properties and Adrenal Depressant Activity of Megestrol Acetate Observed in Castrated Male Rats

Tisell

Salander

1975

Acta Endocrinologica

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Megestrol acetate (17\g=a\-acetoxy-6-dehydro-6-methylprogesterone), a synthetic steroid with high progestational activity, is used in oral contraceptives but also in the treatment of prostatic diseases in man. To investigate whether megestrol acetate has any androgenic properties the growth of the ventral and dorsolateral prostate, the coagulating glands and the seminal vesicles was studied morphologically in castrated rats treated with megestrol acetate and in non-treated castrated rats. The effect of megestrol acetate on the body weight, the levator ani muscle and the adrenals was also studied. Megestrol acetate was administered in daily doses of 0.02 mg, 0.2 mg, 2.0 mg or 20.0 mg for a period of 21 days. Megestrol acetate in the two higher doses retarded growth and gave a low weight for the levator ani muscle at autopsy indicating an anti-anabolic or catabolic action of megestrol acetate in high doses. Megestrol acetate in daily doses of 0.2, 2.0 and 20.0 mg caused an involution of the adrenal glands. After the two higher doses the weight of the adrenals amounted to only about a third of that of the untreated rats.Megestrol acetate in the lower doses had no demonstrable effect on the growth of the accessory reproductive glands. After the two higher doses of megestrol acetate some growth of the dorsal part of the dorsolateral prostate and of the coagulating glands was observed. Only the seminal vesicles exhibited complete morphological criteria of an androgenic stimulation and then only after the largest dose of megestrol acetate. The investigation shows that megestrol acetate has weak androgenic properties which are apparent at a dose per kg body weight approximately 200 times greater than that used in the treatment of prostatic diseases in man.

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Section: Discussionsupporting

confidence: 47%

Androgenic Properties and Adrenal Depressant Activity of Megestrol Acetate Observed in Castrated Male Rats

Tisell

Salander

1975

Acta Endocrinologica

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“…at the vaginal end-point. As to 6a-methyl-17a-acetoxyprogesterone and 17oc-ethynyl-19-nor¬ testosterone, some comparative data can be found in the literature about their oestrogen-antagonistic effects at the uterine level (Edgren, Calhoun, Elton & Colton, 1959;Elton, Edgren & Calhoun, 1960). Since, however, no data are available about the relative ability of either the parent compounds or their cyclopentyl enol ethers to counteract oestrogens at the vaginal level, the last hypothesis must await further studies to be proved or disproved.…”

Section: Resultsmentioning

confidence: 92%

Studies on Steroidal Enol Ethers: Antigonadotrophic Activity of Cyclopentyl Derivatives of Some Orally Active Progestins

Falconi¹,

Bruni²

1962

Journal of Endocrinology

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Cyclopentyl enol ethers of some orally active progestational steroids have been compared with their parent compounds for their ability to inhibit hypersecretion of pituitary gonadotrophin in parabiotic rats (intact female\p=m-\ castrated male). Although in previous experiments enolic etherification altered the 'antioestrus' activity it did not change the antigonadotrophic potency either of 6\g=a\-methyl-17\g=a\-acetoxyprogesterone or 17\g=a\-ethynyl \x=req-\ 19-nortestosterone acetate. The lack of parallelism between antigonadotrophic and 'antioestrus' activities is discussed.

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“…Medroxyprogesterone acetate MPA (17α-hydroxy-6α-methylprogesterone acetate) is a synthetic derivative of progesterone that is also more potent than progesterone. 55 MPA also acts as an agonist of the androgen and glucocorticoid receptors, although its affinity for the androgen and glucocorticoid receptors is much lower than that of MA. 56 its half-life is 12-17 h following an oral dose and 40-50 days following an intramuscular (iM) dose.…”

Section: Low Dosagementioning

confidence: 99%

Progestins to control feline reproduction

Romagnoli

2015

Journal of Feline Medicine and Surgery

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Biological Activities of Some 6-Methylated Progesterones.

Abstract: 175the chick comb in animals not treated with androgen were significnatly reduced by administration of this compound. A-norprogesterone is not androgenic, estrogenic, anti-estrogenic, progestational or an ti-proges ta tional under the experimental conditions described.

Cited by 22 publications

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Androgenic Properties and Adrenal Depressant Activity of Megestrol Acetate Observed in Castrated Male Rats

Androgenic Properties and Adrenal Depressant Activity of Megestrol Acetate Observed in Castrated Male Rats

Studies on Steroidal Enol Ethers: Antigonadotrophic Activity of Cyclopentyl Derivatives of Some Orally Active Progestins

Progestins to control feline reproduction

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