17β-Hydroxyestra-4,9,11-trien-3-one (trenbolone) exhibits tissue selective anabolic activity: effects on muscle, bone, adiposity, hemoglobin, and prostate
| Autor: | Darryl F. Cannady, John M. Hance, Jennifer E. Pingel, Cesar A. Santillana, Stephen E. Borst, Judyta A. Lipinska, Bryan P. Conrad, Joshua F. Yarrow, Joshua Sanchez, Tisha D. VanPelt, Sean C. McCoy, Christine F. Conover, Thomas J. Wronski |
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| Rok vydání: | 2011 |
| Předmět: |
Male
medicine.medical_specialty Anabolism Hormone Replacement Therapy Physiology medicine.drug_class Endocrinology Diabetes and Metabolism Drug Evaluation Preclinical Pilot Projects Biology Bone and Bones Hemoglobins Anabolic Agents Trenbolone Prostate Physiology (medical) Internal medicine medicine Animals Testosterone Orchiectomy Adiposity Muscles Organ Size Articles Androgen Rats Inbred F344 Rats Androgen receptor Endocrinology medicine.anatomical_structure Selective androgen receptor modulator Organ Specificity Trenbolone Acetate medicine.drug |
| Zdroj: | American Journal of Physiology-Endocrinology and Metabolism. 300:E650-E660 |
| ISSN: | 1522-1555 0193-1849 |
| DOI: | 10.1152/ajpendo.00440.2010 |
| Popis: | Selective androgen receptor modulators (SARMs) now under development can protect against muscle and bone loss without causing prostate growth or polycythemia. 17β-Hydroxyestra-4,9,11-trien-3-one (trenbolone), a potent testosterone analog, may have SARM-like actions because, unlike testosterone, trenbolone does not undergo tissue-specific 5α-reduction to form more potent androgens. We tested the hypothesis that trenbolone-enanthate (TREN) might prevent orchiectomy-induced losses in muscle and bone and visceral fat accumulation without increasing prostate mass or resulting in adverse hemoglobin elevations. Male F344 rats aged 3 mo underwent orchiectomy or remained intact and were administered graded doses of TREN, supraphysiological testosterone-enanthate, or vehicle for 29 days. In both intact and orchiectomized animals, all TREN doses and supraphysiological testosterone-enanthate augmented androgen-sensitive levator ani/bulbocavernosus muscle mass by 35–40% above shams ( P ≤ 0.001) and produced a dose-dependent partial protection against orchiectomy-induced total and trabecular bone mineral density losses ( P < 0.05) and visceral fat accumulation ( P < 0.05). The lowest doses of TREN successfully maintained prostate mass and hemoglobin concentrations at sham levels in both intact and orchiectomized animals, whereas supraphysiological testosterone-enanthate and high-dose TREN elevated prostate mass by 84 and 68%, respectively ( P < 0.01). In summary, low-dose administration of the non-5α-reducible androgen TREN maintains prostate mass and hemoglobin concentrations near the level of shams while producing potent myotrophic actions in skeletal muscle and partial protection against orchiectomy-induced bone loss and visceral fat accumulation. Our findings indicate that TREN has advantages over supraphysiological testosterone and supports the need for future preclinical studies examining the viability of TREN as an option for androgen replacement therapy. |
| Databáze: | OpenAIRE |
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