Effect of Desoxycorticosterone and its Esters

Miescher, K.; Fischer, Werner; Tschopp, E.

doi:10.1038/142435b0

Cited by 28 publications

(6 citation statements)

References 3 publications

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“…The difficulty in the case of deoxycorticosterone acetate ('DCA'), however, was that this substance by itself produces a progestational reaction in the rabbit in doses of 5-10 mg., which are only 5-10 times greater than the required amount of progesterone [Miescher, Fischer & Tschopp, 1938;Robson, 1939]. Conversion of DCA to pro¬ gesterone could thus be demonstrated biologically only if the percentage conversion was of a high order, giving rise to marked increase in progestational effect.…”

mentioning

confidence: 98%

The Conversion of Pregnenolone to a More Active Progestational Substance by Incubation With Endocrine Tissues in Vitro

Nissim¹,

Robson²

1952

J Endocrinol

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Incubation of pregnenolone with minced beef corpora lutea resulted in conversion of the steroid to a more active progestational substance as shown by biological assay on the endometrium of the spayed rabbit. Control studies with non-incubated pregnenolone and corpus luteum incubated without steroid, injected separately and in combination, all yielded negative results.To exclude bacterial action, experiments were repeated under sterile conditions, but without diminution in conversion activity.Negative results were obtained when pregnenolone was incubated with spleen, liver or ovaries. The incubation of this steroid with beef adrenal and human placenta, however, resulted in active conversion.It is noteworthy that the adrenal appears to be even more active in the conversion of pregnenolone than the corpus luteum. The association exhibited by the adrenal gland of a lower progesterone content and greater conversion activity, as compared with the corpus luteum, points to progesterone as a likely intermediate substance in the synthesis of the adrenal corticoids.

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mentioning

confidence: 98%

The Conversion of Pregnenolone to a More Active Progestational Substance by Incubation With Endocrine Tissues in Vitro

Nissim¹,

Robson²

1952

J Endocrinol

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“…These findings were taken to mean that the two hormones were inactivated during transport through the liver via the portal circula¬ tion, but the experiment did not exclude the possibility that the spleen itself played some role in the inactivation. Methyltestosterone, however, first shown to be a potent androgen in 1935 by Ruzicka, Goldberg & Rosenberg, is unequivocally more potent than any other androgen when administered orally to castrated rats [Miescher & Tschopp, 1938], and it has been claimed that the presence of the methyl group in the 17 position protected this androgen from destruction in the stomach and intestine. Biskind [1940] concluded that its activity when given by mouth was due to absorption via the lymphatics.…”

mentioning

confidence: 98%

A Comparison of the Relative Efficacy of Methyltestosterone by the Gastric and Oral Transmucosal Routes

Foss¹

1956

Journal of Endocrinology

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An attempt has been made to compare the relative efficacy of two methods of medication with methyltestosterone, namely by absorption through the oral mucosa from slowly soluble tablets and by ingestion.The method of comparison adopted was to estimate the extent to which menstruation was postponed after giving 25 mg methyltestosterone twice daily for 30 days from the onset of bleeding. The effectiveness of the two routes of administration was compared in the same individual.The results indicate that buccal absorption is slightly more effective than ingestion.Biskind & Mark [1939] found that, when pellets of testosterone propionate and oestrone were implanted respectively into the spleens of castrate male and female rats, the hormones did not exert their characteristic effect. They did so, however, when the spleens containing the pellets were transplanted subcutaneously and the splenic artery and vein ligated. These findings were taken to mean that the two hormones were inactivated during transport through the liver via the portal circula¬ tion, but the experiment did not exclude the possibility that the spleen

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“…The disadvantage of these preparations is that they are largely inactive when taken by mouth, owing to their destruction by the liver. An advance in treatment followed the production of methyltestosterone, which, when given orally, was shown to be active in castrated rats (Miescher and Tschopp, 1938), and later its potency was confirmed in man. Taken in this way, only about one-third is destroyed by-the liver, but this is sufficient to make oral therapy expensive.…”

mentioning

confidence: 99%

Fluoxymesterone

Rm¹

1959

BMJ

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Effect of Desoxycorticosterone and its Esters

Cited by 28 publications

References 3 publications

The Conversion of Pregnenolone to a More Active Progestational Substance by Incubation With Endocrine Tissues in Vitro

The Conversion of Pregnenolone to a More Active Progestational Substance by Incubation With Endocrine Tissues in Vitro

A Comparison of the Relative Efficacy of Methyltestosterone by the Gastric and Oral Transmucosal Routes

Fluoxymesterone

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