Tissue selectivity and potential clinical applications of trenbolone (17β-hydroxyestra-4,9,11-trien-3-one): A potent anabolic steroid with reduced androgenic and estrogenic activity

@article{Yarrow2010TissueSA,
  title={Tissue selectivity and potential clinical applications of trenbolone (17$\beta$-hydroxyestra-4,9,11-trien-3-one): A potent anabolic steroid with reduced androgenic and estrogenic activity},
  author={Joshua F Yarrow and Sean C. McCoy and Stephen E. Borst},
  journal={Steroids},
  year={2010},
  volume={75},
  pages={377-389}
}
Recently, the development of selective androgen receptor modulators (SARMs) has been suggested as a means of combating the deleterious catabolic effects of hypogonadism, especially in skeletal muscle and bone, without inducing the undesirable androgenic effects (e.g., prostate enlargement and polycythemia) associated with testosterone administration. 17beta-Hydroxyestra-4,9,11-trien-3-one (trenbolone; 17beta-TBOH), a synthetic analog of testosterone, may be capable of inducing SARM-like effects… Expand
17β-Hydroxyestra-4,9,11-trien-3-one (trenbolone) exhibits tissue selective anabolic activity: effects on muscle, bone, adiposity, hemoglobin, and prostate.
TLDR
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. Expand
17β-Hydroxyestra-4,9,11-trien-3-one (Trenbolone) preserves bone mineral density in skeletally mature orchiectomized rats without prostate enlargement.
TLDR
In skeletally mature rodents, both high-dose TE and low-dose TREN completely prevented the ORX-induced loss of tBMD at the distal femoral metaphysis and increased LABC mass. Expand
17β-trenbolone, an anabolic-androgenic steroid as well as an environmental hormone, contributes to neurodegeneration.
TLDR
17β-trenbolone accumulated in adult rat brain, especially in the hippocampus, and in the fetus brain and altered Aβ42 accumulation and played critical roles in neurodegeneration. Expand
Novel Uses for the Anabolic Androgenic Steroids Nandrolone and Oxandrolone in the Management of Male Health
TLDR
A brief review of the history of AAS is provided and clinical applications of two of the more well-known AAS: n androlone and oxandrolone are discussed, which exhibit favorable myotrophic/androgenic ratios and have been investigated for effectiveness in numerous disease states. Expand
University of Szeged Department of Pharmacodynamics and Biopharmacy CHARACTERIZATION OF ANTINEOPLASTIC PROPERTIES OF NOVEL ANDROSTANE-BASED SYNTHETIC STEROIDS PhD Thesis
Novel 16-hydroxymethyl-19-nortestosterone diastereomers were prepared by Birch reduction from the corresponding 3-methoxy-16-hydroxymethylestra-1,3,5(10)-trien-17-ol isomers with knownExpand
Stereocontrolled synthesis of the four 16-hydroxymethyl-19-nortestosterone isomers and their antiproliferative activities
TLDR
The results indicated that 17α-19-nortestosterone selectively disturbs the viability of HeLa cells without greatly affecting other cancer cell types and intact fibroblasts. Expand
Transcriptional regulation of myotrophic actions by testosterone and trenbolone on androgen-responsive muscle
Androgens regulate body composition and skeletal muscle mass in males, but the molecular mechanisms are not fully understood. Recently, we demonstrated that trenbolone (a potent syntheticExpand
Toxic impact of Anabolic Androgenic Steroids in Primary Rat Cortical Cell Cultures
TLDR
Overall, it is found that supra-physiological concentrations of AASs induce cell death in mixed primary cortical cultures, but to different extents, and possibly through various mechanisms. Expand
Beck: Aromatase and Testosterone Administration
TLDR
In conclusion, androgens are able to induce direct effects on musculoskeletal and adipose tissue, independent of aromatase activity, as well as producing potent myotrophic effects in the LABC muscle and maintained fat-mass at the level of Shams. Expand
Medicinal Use of Testosterone and Related Steroids Revisited
TLDR
Although these agents are currently regarded as rather older generation drugs and their use may lead to serious side-effects, they still have medicinal value as androgenic, anabolic, and even anti-androgenic agents. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 274 REFERENCES
Steroidal androgens and nonsteroidal, tissue-selective androgen receptor modulator, S-22, regulate androgen receptor function through distinct genomic and nongenomic signaling pathways.
TLDR
Comparisons and in vitro studies reveal novel differences in the molecular mechanisms by which S-22, a nonsteroidal SARM, and DHT mediate their pharmacological effects. Expand
Bone anabolic effects of S-40503, a novel nonsteroidal selective androgen receptor modulator (SARM), in rat models of osteoporosis.
TLDR
Collectively, this novel compound served as a prototype for SARMs, which had unique tissue selectivity with high potency for bone formation and lower impact upon sex accessory tissues. Expand
Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5alpha-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: new approach for benign prostate hyperplasia.
TLDR
Although S-1 and finasteride showed very similar suppressive effects in the prostate of intact male rats, they decreased prostate size via different mechanisms of action, indicating that SARMs may demonstrate clinical utility as single agent or combination therapy for BPH. Expand
Characterisation of the affinity of different anabolics and synthetic hormones to the human androgen receptor, human sex hormone binding globulin and to the bovine progestin receptor
TLDR
It is concluded that MGA and TBA metabolites may be hor‐monally active substances, which will be present in edible tissues and in manure, and detailed investigations on biodegradation, distribution and bio‐efficacy of these substances are necessary. Expand
Different patterns of metabolism determine the relative anabolic activity of 19-norandrogens
Testosterone, the principal androgen secreted by Leydig cells, exerts a wide range of actions including growth of the male reproductive tract (androgenic effects) and growth of non-reproductiveExpand
Dimethandrolone (7α,11β-dimethyl-19-nortestosterone) and 11β-methyl-19-nortestosterone are not converted to aromatic A-ring products in the presence of recombinant human aromatase
TLDR
Data support the notion that in the absence of the C19-methyl group, aromatization of androgenic substrates proceeds slowly or not at all and that this reaction is impeded by the presence of a methyl group at the 11beta position. Expand
Effects of the androgenic growth promoter 17-beta-trenbolone on fecundity and reproductive endocrinology of the fathead minnow.
TLDR
The studies indicate that 17-beta-trenbolone is a potent androgen and reproductive toxicant in fish and further studies are warranted to assess potential ecological risk. Expand
Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats.
TLDR
The potent oral activity and tissue selectivity exhibited by BMS-564929 are expected to yield a clinical profile that provides the demonstrated beneficial effects of T in muscle and other tissues with a more favorable safety window. Expand
Selective non-steroidal inhibitors of 5 alpha-reductase type 1.
TLDR
This paper will review the major classes of 5 alpha R inhibitors focusing in particular on non-steroidal inhibitors and on structural features that enhance the selectivity versus the type 1 isozyme. Expand
Selective non-steroidal inhibitors of 5α-reductase type 1
TLDR
This paper will review the major classes of 5αR inhibitors focusing in particular on non-steroidal inhibitors and on structural features that enhance the selectivity versus the type 1 isozyme. Expand
...
1
2
3
4
5
...