5/3-Androsterone effects

The main use of progestins is based on their antifertility effect. Since progesterone is poorly absorbed, it cannot be given orally furthermore, it is not particularly potent and has an unacceptably short serum half-life of about 5 minutes. In early work, ethis-terone (5.39), an acetylenic compound prepared from androsterone, was an orally active progestin, but also had male hormone action. In subsequent work, a large number of... 

Force-field calculations have given the atomic co-ordinates for 3a-hydroxy-5a-androstan-17-one ( androsterone ) with about the same accuracy as X-ray measurements, the errors being no greater than 0.1 A. The value of this method lies partly in its speed (10 minutes of IBM 360 computer time) and partly in the fact that no crystal is required. Variations of energy with conformation can also be computed. The authors stress the likely dangers in using Dreiding models, which may differ markedly in shape from actual molecules because they fail to simulate torsional and van der Waals effects. 

Like single-component isotherms, competitive isotherms depend on the composition of the mobile phase and the temperature [10]. Figure 4.11 [10] illustrates for a 1 1 mixture of ds- and trans-androsterone the effects of the mobile phase composition and temperature, respectively, on the adsorption isotherm. The general trend is for adsorption to decrease with increasing concentration of the strong solvent and with increasing temperature. These experimental parameters must be... 

Figure 4.11 Effect of the experimental conditions on the competitive isotherm of cis-and trans-androsterone (1 1 mixture). Experimental data ds-androsterone, A, trans-androsterone, two-term LeVan-Vermeulen isotherm ds-androsterone, dotted line, trans-androsterone solid line. (Left) Effect of the mobile phase composition. (Right) Effect of the temperature. Reproduced with permission from S. Golshan-Shirazi, J.-X. Huang and G. Guiochon, Anal. Chem., 63 (1991) 1147 (Figs. 3 and 4), 1991 American Chemical Society.

Initially, it had been thought that clofibrate may have ehcited a favorable hypohpidemic activity in the rat predominantly through stimulation of the hypocholesterolemic action of endogenous androsterone [270]. In addition, clofibrate itself was found to elevate rather than depress serum hpid levels in the male rhesus monkey and its hypohpidemic effect was observed only following simultaneous oral administration of (Cl) and androsterone in this species [272]. For these reasons a combination of clofibrate and androsterone was employed in the initial clinical trials. 

Gallagher and co-workers [389] have emphasized that metabolites of corticoid hormones are not simply inactive end-products of a spent hormone ready for elimination, but may have their own important metabohc functions. Thus, androsterone, an end-metabohte of androgens, is an effective endogenous hypocholesterolemic hormone. Moreover, the production of androsterone is increased as one of the results of thyroxine action hence, this androgen meta-... 

A metabohte of 17a-methyltestosterone, compound CLXXXII, has been reported to possess in the dog at doses below 1 mg/kg/day [406], more potent hypocholesterolemic activity than 17a-methyltestosterone. Compound CLXXXIII (SC-12,790) [407] has been found to possess as high oral hypocholesterolemic activity as androsterone given parenterally to rats rendered hypercholesterolemic with 6-propylthiouracil [408]. Substance CLXXXIII showed no effect on cholesterol biosynthesis from mevalonate in the liver, but enhanced cholesterol excretion in the bile of rats [409]. It is worthy of note that the 3jS-epimer of CLXXXIII was found to lack significant hypocholesterolemic activity even at doses as high as 10 mg/kg [407]. 

Effective Adsorption of Dehydroepi-androsterone (DHA) Sulfate and Other 17-Ketosteroid Conjugates from Urine by Amberlite Clin. Biochem. 4(4) 287-296 (1971) ... 

Howard, R. P., P. Alaupovic, 0. J. Brusco, and R. H. Furman Effects of ethyl chlo-rophenoxyisobutyrate, alone or with androsterone (Atromid) on serum lipids, lipoproteins and related metabolic parameters in normal and hyperlipidemic subjects. J. Atheroscler. Res. 3, 482 (1963). 

The Pituitary Control of Testicular Activity.—Gonadotropic hormones secreted by the anterior pituitary control (i.) the descent of the testicle, (ii.) the onset and maintenance of spermatogenesis, and (iii.) the output of the androgens, this last effect being homologous with the action of FSH in the female. Pituitary gonadotropic activity is in abeyance before puberty, as shown by the absence of androsterone from the urine. 

Atromid, a combination of clofibrate and androsterone, was found to be effective in humans for lowering serum cholesterol, triglyceride, and phospholipid levels,cholesterol and total lipids, (but not platelet stickiness), and cholesterol, phospholipid and befa-lipoproteins. 

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