Estrogen Antagonisms: The Effects of a Series of Relatives of 19-Nortestosterone on Estrone-Induced Uterine Growth

Edgren, Richard A.; Calhoun, David W.; Elton, Richard L.; Colton, Frank B.

doi:10.1210/endo-65-2-265

Cited by 51 publications

(11 citation statements)

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“…Pituitary ACTH concentration was significantly diminished in all groups receiving SC9686 but pituitary atrophy was observed only in rats receiving SC9686 for 14 days. Adrenal glands were found to be atrophied as well as depressed functionally when 6-methyl-17-acetoxyprogesterone was injected into male rats which were subsequently challenged with cold shock, as shown by Edgren, Hambourger and Calhoun (4). Although atrophy of the adrenal gland can occur in animals following the administration of compounds with biochemical properties similar to that of MPA, as shown above, we did not observe clinically significant adrenocortical suppression in the patients we studied.…”

Section: Discussionsupporting

confidence: 64%

“…In addition to its effects on pituitary-gonadal function, there is evidence to suggest that MPA may also have some influence on the pituitaryadrenocortical axis. In animal experiments, MPA has produced adrenocortical atrophy in rats (4), and in man it has been shown to have a cortisone-like action in adrenalectomized subjects (5). In man, however, its effect on pituitary-adrenocortical function remains controversial.…”

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confidence: 99%

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Pituitary-Adrenal Function in Ten Patients Receiving Medroxyprogesterone Acetate for True Precocious Puberty

Mathews

Abrams

Morishima

1970

The Journal of Clinical Endocrinology & Metabolism

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The effect of medroxyprogesterone acetate (MPA) on pituitary-adrenal function was investigated in 10 patients with true precocious puberty. Although the patients receiving MPA responded to exogenously administered ACTH by a rise in the plasma 17-hydroxycorticosteroids, the mean values of both the pre-and post-ACTH levels were statistically lower than those obtained in the controls. In 7 of the 8 patients the increase of the urinary 17-ketogenic steroids following the oral administration of metyrapone was less than 2-fold. The data suggest that MPA in the dosages tested has a suppressive effect on pituitary ACTH synthesis and/ or release. Despite this inhibition, however, no clinical evidence of hypoadrenocorticism was observed in these patients even during periods of stress. When the drug was discontinued, pituitary-adrenal function rapidly returned toward normal, suggesting that the suppressive effect of MPA was a relatively mild one. (J Clin Endocr 30: 653,1970)

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Section: Discussionsupporting

confidence: 64%

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confidence: 99%

Pituitary-Adrenal Function in Ten Patients Receiving Medroxyprogesterone Acetate for True Precocious Puberty

Mathews

Abrams

Morishima

1970

The Journal of Clinical Endocrinology & Metabolism

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“…The myotrophic to androgenic ratios 441 Other biological properties of these compounds have been studied by subcutaneous administration. All compounds were weakly uterotrophic in the mouse uterine weight assay (6) with relative potencies ranging from 0.02 to 0.03% of estrone. Progestational activity of compounds II, III and IV in rabbits by means of the Clauberg assay (7) and relative potencies of 0.1, 0.1 and 100 times progesterone, respectively, were obtained.…”

Section: Resultsmentioning

confidence: 99%

Estradienes and 2-Oxaestradienes. Potent Oral Anabolic-Androgenic Agents

Nutting¹,

Calhoun²

1969

Endocrinology

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Anabolic and myotrophic properties of a series of estradienes were assessed by bioassay in castrated rats employing 17a-methyltestosterone (MT) as the standard. The weights of the seminal vesicles and ventral lobe of the prostate glands were used as independent indicators of androgenic activity. Anabolic activity was determined from the weights of the levator ani muscle. The compounds studied were 17j8-hydroxyestra-4,9(10)-dien-3-one (I), 17a-methyl-17/3-hydroxyestra-4,9(10)-dien-3-one (II), 17/3-hydroxy-2-oxaestra-4,9(10)-dien-3-one (III), and 17a-methyl-l7j3-hydroxy-2-oxaestra-4,9(10)-dien-3-one (IV). The androgenic acitivity of the parent compound (I), estimated by both parameters, was slightly less than the standard, while the myotrophic activities for the test and standard compounds were approximately equal. The 17a-methyl derivative (II) had androgenic and myotrophic relative potencies of 5-7 and 80 times MT, respectively. The 2-oxa analog (III) was 2-9 times as androgenic as MT and 93 times as myotrophic. Activity of this magnitude was surprising in view of the absence of a methyl substituent on C-17 of this compound. The 17a-methyl-2-oxa derivative (IV) was by far the most potent compound tested, being 22-47 times more androgenic and 550 times more myotrophic than MT. Both the 2-oxa (III) and 17a-methyl-2-oxa (IV) derivatives possessed highly favorable myotrophic: androgenic ratios ranging from 11 to 37 (III) or 12 to 25 (IV), respectively, depending on the androgenic organ used in the calculation. (Endocrinology 84: 441, 1969)

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“…Anti-oestrogenie effects 1. Anti-uterotrophic activity in the mouse was measured according to the test de¬ scribed by Edgren et al (1959). Oestradiol monobenzoate (OeB) was used.…”

Section: A Animal Studiesmentioning

confidence: 99%

Endocrine Effects of Two New Retro-Steroids in Animal Models and in Women

Morsink

Wachter

Brenner

et al. 1976

European Journal of Endocrinology

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The hormonal properties of two retro-steroids, DU 41 164 and DU 41 165, have been investigated in animal models and in clinical studies. Chlormadinone acetate (CMA) was used as a reference standard in the animal experiments. Both retro-steroids exihibited high progestational activity in the rabbit; their potency was 18 times that of CMA when given orally.Both retro-steroids maintained pregnancy in rabbits and rats when administered orally; in rabbits the potencies of DU 41 164 and DU 41 165 were respectively 6 and 11 times the potency of CMA. In the pregnancy maintenance test in rats the ED 50 of DU 41 164 was 2000 \g=m\g/kg/d and that of DU 41 165 was 290 \g=m\g/kg/d,whereas CMA could not maintain pregnancy when given in doses of 50 000 \ g = m\ g / k g / d . Both DU 41 164 and DU 41 165 were highly active as antifertility agents in rabbits and rats. When given orally, their potencies in rabbits were respectively 80 and 40 times that of CMA, whereas in rats their potencies were respectively 100 and 300 times that of CMA. In the ovulation inhibition test in rabbits, the ED 50 values of orally administered DU 41 164 and DU 41 165 were 0.5 and 0.4 \g=m\g/kg,respectively, whereas the ED 50 of CMA was 40 \g=m\g/kg. In rats, depending on the day of the cycle on which administered, the retro-steroids given orally either inhibited or induced ovulation. In the

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Estrogen Antagonisms: The Effects of a Series of Relatives of 19-Nortestosterone on Estrone-Induced Uterine Growth

Cited by 51 publications

References 0 publications

Pituitary-Adrenal Function in Ten Patients Receiving Medroxyprogesterone Acetate for True Precocious Puberty

Pituitary-Adrenal Function in Ten Patients Receiving Medroxyprogesterone Acetate for True Precocious Puberty

Estradienes and 2-Oxaestradienes. Potent Oral Anabolic-Androgenic Agents

Endocrine Effects of Two New Retro-Steroids in Animal Models and in Women

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