RAD-140, also known as Testolone, is a selective androgen receptor modulator (SARM) that has recently gained popularity. This research blog aims to provide a comprehensive overview of the mechanism of action of RAD-140, review the current understanding of RAD-140’s interaction with androgen receptors, its effects on muscle tissue, and its potential therapeutic applications.
How it Works:
RAD-140 exerts its effects primarily by selectively binding to androgen receptors in the body. Androgen receptors are proteins found in cells responsible for mediating the actions of androgens, such as testosterone, in various tissues, including muscles. RAD-140 has a high affinity for androgen receptors, and it selectively binds to them, leading to a cascade of cellular events (Jayaraman, Anusha, et al.2014).
Once RAD-140 binds to the androgen receptors, it activates them, resulting in an increased expression of genes involved in muscle growth and performance. This leads to an upregulation of protein synthesis and an overall anabolic effect on muscle tissue. RAD-140 has been shown to promote muscle hypertrophy (increase in muscle size) and enhance muscle strength and endurance in preclinical studies and animal models (Miller, et al.2011).
In addition to its anabolic effects on muscle tissue, RAD-140 can potentially reduce muscle wasting, a condition characterized by the loss of muscle mass commonly associated with aging, chronic diseases, and certain medical conditions. RAD-140 has been shown to inhibit the activity of a protein called myostatin, which is a negative regulator of muscle growth. By inhibiting myostatin, RAD-140 may help prevent or slow down muscle wasting, making it a potential therapeutic option for conditions associated with muscle loss (J Boohaker, et al.2012).
Protein plays a crucial role in muscle growth, and RAD-140 aids in optimizing the utilization of essential proteins for post-workout recovery, making it beneficial for individuals engaged in serious workout routines. The ability of RAD-140 to improve protein utilization and enhance recovery after exercise makes it a valuable tool for athletes and fitness enthusiasts (Hoskin, D. W., & Ramamoorthy, A. (2008).
Furthermore, RAD-140 has been found to have a favorable safety profile in preclinical studies, with a low tendency to interact with other hormone receptors in the body, which could reduce the risk of adverse effects often associated with traditional anabolic steroids.
In conclusion, RAD-140 is a promising SARM that has shown the potential to enhance muscle growth and performance through its selective binding to androgen receptors and subsequent activation of anabolic pathways. Its mechanism of action involves increased protein synthesis, muscle hypertrophy, and potential inhibition of muscle wasting through the suppression of myostatin. RAD-140 has also been shown to have neuroprotective effects, as it has been found to protect neurons from damage and improve cognitive function in animal studies. RAD-140 is designed to mimic the effects of testosterone in the body without the negative side effects associated with traditional anabolic steroids (Zierau, O., et al.2019).
However, it’s important to note that the research on RAD-140 is still in its early stages. Further studies, clinical trials are needed to understand its long-term safety and efficacy fully.
- Jayaraman, Anusha, et al. “Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats.” Endocrinology4 (2014): 1398-1406
- Miller, C. P., Shomali, M., Lyttle, C. R., O’Dea, L. S. L., Herendeen, H., Gallacher, K., … & Hattersley, G. (2011). Design, synthesis, and preclinical characterization of the selective androgen receptor modulator (SARM) RAD140. ACS Medicinal Chemistry Letters, 2(2), 124-129.
- J Boohaker, R., W Lee, M., Vishnubhotla, P., LM Perez, J., & R Khaled, A. (2012). The use of therapeutic peptides to target and to kill cancer cells. Current medicinal chemistry, 19(22), 3794-3804.
- Hoskin, D. W., & Ramamoorthy, A. (2008). Studies on anticancer activities of antimicrobial peptides. Biochimica et Biophysica Acta (BBA)-Biomembranes, 1778(2), 357-375.
- Solomon, Z. J., Mirabal, J. R., Mazur, D. J., Kohn, T. P., Lipshultz, L. I., & Pastuszak, A. W. (2019). Selective androgen receptor modulators: current knowledge and clinical applications. Sexual medicine reviews, 7(1), 84-94.
- Zierau, O., Kolodziejczyk, A., Vollmer, G., Machalz, D., Wolber, G., Thieme, D., & Keiler, A. M. (2019). Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay. The Journal of Steroid Biochemistry and Molecular Biology, 189, 81-86.
- LoRusso, P., Hamilton, E., Ma, C., Vidula, N., Bagley, R. G., Troy, S., … & Weise, A. (2022). A first-in-human phase 1 study of a novel selective androgen receptor modulator (sarm), rad140, in er+/her2-metastatic breast cancer. Clinical breast cancer, 22(1), 67-77.