Sodium-retaining activity of some natural and synthetic 21-deoxysteroids
The effect of progesterone and six other C21 -deoxysteroids on renal sodium retention by male adrenaleotomized rats was compared with the effect exerted by the natural corticoids aldosterone, 11-deoxycorticosterone, and corticosterone. Steroids were active in the following order: aldosterone > 11...
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1995
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| Acceso en línea: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0026895X_v47_n3_p535_Burton http://hdl.handle.net/20.500.12110/paper_0026895X_v47_n3_p535_Burton |
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paper:paper_0026895X_v47_n3_p535_Burton2023-06-08T14:53:55Z Sodium-retaining activity of some natural and synthetic 21-deoxysteroids 11,19 oxidoprogesterone 11beta,17beta dihydroxy 6 methyl 17alpha (1 propynyl)androsta 1,4,6 trien 3 one 21 deoxycorticosterone 5alpha pregnane 3,20 dione 6,19 oxido 11 oxoprogesterone 6,19 oxidoprogesterone aldosterone corticosterone deoxycorticosterone mineralocorticoid receptor pregnanedione progesterone progesterone derivative transcortin unclassified drug adrenalectomy animal experiment animal tissue article controlled study dose response drug conformation drug half life intramuscular drug administration intraperitoneal drug administration male nonhuman potassium urine level priority journal rat receptor affinity sodium retention sodium urine level subcutaneous drug administration Adrenal Glands Adrenalectomy Aldosterone Animal Comparative Study Cytosol Desoxycorticosterone Half-Life Kidney Male Molecular Conformation Potassium Progesterone Rats Rats, Sprague-Dawley Receptors, Steroid Sodium Steroids Support, Non-U.S. Gov't Tritium The effect of progesterone and six other C21 -deoxysteroids on renal sodium retention by male adrenaleotomized rats was compared with the effect exerted by the natural corticoids aldosterone, 11-deoxycorticosterone, and corticosterone. Steroids were active in the following order: aldosterone > 11,19-oxidoprogesterone > 5αH-3,20-pregnanedione ≥ 5βH-3,20-pregnanedione > progesterone = 11-ketoprogesterone > 6,19-oxidoprogesterone = 11-keto- 6,19-oxidoprogesterone ≥ corticosterone. All C21-deoxysteroids, except 11,19-oxidoprogesterone, exhibited parabolic log dose-response functions, indicating an effect that opposes renal sodium retention at high doses. 11,19-Oxidoprogesterone and the natural corticoids exhibited normal, exponential, log dose-response curves. Diverse geometric parameters related to molecular planarity were calculated and their correlation with biopharmacological properties was attempted. The best linear regression was obtained for correlation of the concavity of log dose-response parabolas (second-order coefficients) of C21-deoxysteroids with the C3=O/ring D angle of these molecules. A good linear regression could also be obtained for correlation of the affinity of C21-deoxysteroids, except 11,19- oxidoprogesterone, for purified type I mineralocorticoid receptors with those angles. The latter correlation deteriorated upon incorporation of the affinity data for the three natural corticoids, due to similar affinities of these hormones for type I mineralocorticoid receptors, but could be restored when the binding data for the unpurified, corticosterone-binding globulin- containing stage of the receptors were considered. In vivo binding data followed the same trend as that for unpurified receptors. 1995 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0026895X_v47_n3_p535_Burton http://hdl.handle.net/20.500.12110/paper_0026895X_v47_n3_p535_Burton |
| institution |
Universidad de Buenos Aires |
| institution_str |
I-28 |
| repository_str |
R-134 |
| collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
11,19 oxidoprogesterone 11beta,17beta dihydroxy 6 methyl 17alpha (1 propynyl)androsta 1,4,6 trien 3 one 21 deoxycorticosterone 5alpha pregnane 3,20 dione 6,19 oxido 11 oxoprogesterone 6,19 oxidoprogesterone aldosterone corticosterone deoxycorticosterone mineralocorticoid receptor pregnanedione progesterone progesterone derivative transcortin unclassified drug adrenalectomy animal experiment animal tissue article controlled study dose response drug conformation drug half life intramuscular drug administration intraperitoneal drug administration male nonhuman potassium urine level priority journal rat receptor affinity sodium retention sodium urine level subcutaneous drug administration Adrenal Glands Adrenalectomy Aldosterone Animal Comparative Study Cytosol Desoxycorticosterone Half-Life Kidney Male Molecular Conformation Potassium Progesterone Rats Rats, Sprague-Dawley Receptors, Steroid Sodium Steroids Support, Non-U.S. Gov't Tritium |
| spellingShingle |
11,19 oxidoprogesterone 11beta,17beta dihydroxy 6 methyl 17alpha (1 propynyl)androsta 1,4,6 trien 3 one 21 deoxycorticosterone 5alpha pregnane 3,20 dione 6,19 oxido 11 oxoprogesterone 6,19 oxidoprogesterone aldosterone corticosterone deoxycorticosterone mineralocorticoid receptor pregnanedione progesterone progesterone derivative transcortin unclassified drug adrenalectomy animal experiment animal tissue article controlled study dose response drug conformation drug half life intramuscular drug administration intraperitoneal drug administration male nonhuman potassium urine level priority journal rat receptor affinity sodium retention sodium urine level subcutaneous drug administration Adrenal Glands Adrenalectomy Aldosterone Animal Comparative Study Cytosol Desoxycorticosterone Half-Life Kidney Male Molecular Conformation Potassium Progesterone Rats Rats, Sprague-Dawley Receptors, Steroid Sodium Steroids Support, Non-U.S. Gov't Tritium Sodium-retaining activity of some natural and synthetic 21-deoxysteroids |
| topic_facet |
11,19 oxidoprogesterone 11beta,17beta dihydroxy 6 methyl 17alpha (1 propynyl)androsta 1,4,6 trien 3 one 21 deoxycorticosterone 5alpha pregnane 3,20 dione 6,19 oxido 11 oxoprogesterone 6,19 oxidoprogesterone aldosterone corticosterone deoxycorticosterone mineralocorticoid receptor pregnanedione progesterone progesterone derivative transcortin unclassified drug adrenalectomy animal experiment animal tissue article controlled study dose response drug conformation drug half life intramuscular drug administration intraperitoneal drug administration male nonhuman potassium urine level priority journal rat receptor affinity sodium retention sodium urine level subcutaneous drug administration Adrenal Glands Adrenalectomy Aldosterone Animal Comparative Study Cytosol Desoxycorticosterone Half-Life Kidney Male Molecular Conformation Potassium Progesterone Rats Rats, Sprague-Dawley Receptors, Steroid Sodium Steroids Support, Non-U.S. Gov't Tritium |
| description |
The effect of progesterone and six other C21 -deoxysteroids on renal sodium retention by male adrenaleotomized rats was compared with the effect exerted by the natural corticoids aldosterone, 11-deoxycorticosterone, and corticosterone. Steroids were active in the following order: aldosterone > 11,19-oxidoprogesterone > 5αH-3,20-pregnanedione ≥ 5βH-3,20-pregnanedione > progesterone = 11-ketoprogesterone > 6,19-oxidoprogesterone = 11-keto- 6,19-oxidoprogesterone ≥ corticosterone. All C21-deoxysteroids, except 11,19-oxidoprogesterone, exhibited parabolic log dose-response functions, indicating an effect that opposes renal sodium retention at high doses. 11,19-Oxidoprogesterone and the natural corticoids exhibited normal, exponential, log dose-response curves. Diverse geometric parameters related to molecular planarity were calculated and their correlation with biopharmacological properties was attempted. The best linear regression was obtained for correlation of the concavity of log dose-response parabolas (second-order coefficients) of C21-deoxysteroids with the C3=O/ring D angle of these molecules. A good linear regression could also be obtained for correlation of the affinity of C21-deoxysteroids, except 11,19- oxidoprogesterone, for purified type I mineralocorticoid receptors with those angles. The latter correlation deteriorated upon incorporation of the affinity data for the three natural corticoids, due to similar affinities of these hormones for type I mineralocorticoid receptors, but could be restored when the binding data for the unpurified, corticosterone-binding globulin- containing stage of the receptors were considered. In vivo binding data followed the same trend as that for unpurified receptors. |
| title |
Sodium-retaining activity of some natural and synthetic 21-deoxysteroids |
| title_short |
Sodium-retaining activity of some natural and synthetic 21-deoxysteroids |
| title_full |
Sodium-retaining activity of some natural and synthetic 21-deoxysteroids |
| title_fullStr |
Sodium-retaining activity of some natural and synthetic 21-deoxysteroids |
| title_full_unstemmed |
Sodium-retaining activity of some natural and synthetic 21-deoxysteroids |
| title_sort |
sodium-retaining activity of some natural and synthetic 21-deoxysteroids |
| publishDate |
1995 |
| url |
https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0026895X_v47_n3_p535_Burton http://hdl.handle.net/20.500.12110/paper_0026895X_v47_n3_p535_Burton |
| _version_ |
1768542681213960192 |