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17alpha-methyl testosterone is used widely as a component of hormone replacement therapy. Previous reports have indicated that contrary to , 17alpha-methyl testosterone is not aromatized. However, 17alpha-methyl testosterone still could affect local estrogen formation by regulating aromatase expression or by inhibiting aromatase action. Both possibilities have important clinical implications.
To evaluate the effect of 17alpha-methyl testosterone on the expression and activity of aromatase, we tested the choriocarcinoma Jar cell line, a cell line that express high levels of P450 aromatase, and the macrophage-like THP-1 cells, which express aromatase only after undergoing differentiation. We found that in both cell lines, 17alpha-methyl testosterone inhibits aromatase activity in a dose-related manner. The curve of inhibition parallels that of letrozole and gives complete inhibition at 10(-4) M 17alpha-methyl testosterone, determined by the tritium release assay. 17alpha-methyl testosterone does not have detectable effects on aromatase RNA and protein expression by Jar cells.
Undifferentiated THP-1 cells had no aromatase activity and showed no effect of 17alpha-methyl testosterone, but differentiated THP-1 (macrophage-like) cells had a similar inhibition of aromatase activity by 17alpha-methyl testosterone to that seen in Jar cells. The Lineweaver-Burke plot shows 17alpha-methyl testosterone to be a competitive aromatase inhibitor. Our results show for the first time that 17alpha-methyl testosterone acts as an aromatase inhibitor.
These findings are relevant for understanding the effects of 17alpha-methyl testosterone as a component of hormone replacement therapy. 17alpha-methyl testosterone may, as a functional androgen and orally active steroidal inhibitor of endogenous estrogen production, also offer special possibilities for the prevention/treatment of hormone-sensitive cancers.
It is the same compound as the one in Primobolan Orals (methenolone acetate), both produced by Schering. In this injectable version, an enanthate ester is added to the steroid, which makes for a slow and gradual release from the site of injection. Its length of activity would thus be quite similar to Testosterone enanthate, with blood levels remaining elevated for approximately two weeks. Methenolone itself is a long acting anabolic, with extremely low androgenic properties.
It’s anabolic effect is also quite mild, its potency is considered to be slightly less than Deca Durabolin (nandrolone decanoate) on a milligram for milligram basis. For this reason, Primobolan is most commonly used during cutting cycles when a mass increase is not the main goal. Some athletes do prefer to combine a mild anabolic like “Primo” with bulking drugs such as Dianabol, Anadrol, or testosterone however, presumably to lower the overall androgen dosage and minimize uncomfortable side effects. When choosing between Primobolan versions, the injectable is preferred over the oral, as it is much more cost effective.
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Related product lists:
|Methenolone enanthate (Primo E)||303-42-4|
|Drostanolone Propionate (Masteron P )||521-12-0|
|Drostanolone enanthate (Masteron E)||521-12-0|