What are SARMs? 💊

Selective Androgen Receptor Modulators (SARMs) are a class of therapeutic compounds that possess similar properties to anabolic agents like steroids, but with reduced androgenic properties. This specific binding and their oral bioavailability 💊 is what makes them so appealing. They can essentially modulate the androgen receptors selectively, promoting anabolic effects on bones and muscles without the extensive side effects typically seen with hormone replacement therapy.

The Science Behind SARMs

The androgen receptor (AR) is a type of nuclear receptor that is activated by binding any of the androgenic hormones, primarily testosterone and dihydrotestosterone (DHT), but also other androgens. This receptor plays a crucial role in the complex web of hormonal signaling that influences a wide range of physiological processes.

SARMs function by binding to androgen receptors (ARs) which are located in various tissues throughout the body. Upon binding, SARMs modulate the receptor's activity, which can increase protein synthesis, muscle growth, and bone density. Unlike traditional hormone methods, SARMs selectively target tissues, aiming to reduce the occurrence of side effects. Their selectivity also allows them to potentially treat a host of medical conditions ranging from Muscle Wasting Diseases to Osteoporosis without the negative effects associated with testosterone or other standard anabolic steroids.

SARMS vs. Peptides: Similarities and Differences

Both SARMs and peptides are pivotal in the world of medical research and bodybuilding due to their potential to influence muscle and tissue growth. Here’s how they compare:

• Similarities: Both can be used to enhance muscle growth, improve healing and recovery, and potentially treat specific diseases affecting muscle and bone.

• Differences:

• Mechanism of Action: Peptides typically work by mimicking or influencing natural processes in the body, such as growth hormone release or natural growth factor activity. SARMs, on the other hand, directly bind to androgen receptors, inducing activity that leads directly to muscle and bone growth.

• Selective Nature: While peptides can have targeted effects, SARMs are specifically designed to target and activate the androgen receptors in muscle and bone, minimizing unwanted systemic effects.

Specific Examples of SARMs Pathways and Effects

MK-2866 (Ostarine) - 5-30mg per Day (Ladies take low dose) for 6-8 Weeks

• Pathway: Binds selectively to Muscle and Bone ARs. It modulates the receptor function such that it preferentially triggers the muscle-building pathways while avoiding those which lead to undesirable effects.

• Effect: Enhances muscle growth and strength, improves bone density, and aids in injury recovery with minimal impacts on the prostate and natural hormone levels.

MK-677 (Ibutamoren) - 25mg per Day for 8 Weeks

• Pathway: Targets ghrelin receptors and mimics ghrelin, stimulating the pituitary to release growth hormone.

• Effect: Increases in muscle mass and bone density, improved metabolism, and enhanced recovery and regeneration of tissues. It works synergistically with the body’s natural growth hormone without directly affecting the androgen receptors.

LGD-4033 (Ligandrol) - 5-10mg per Day for 6 Weeks

• Pathway: Exhibits a high affinity for muscle and bone ARs, acting predominantly in these tissues with reduced activity in the sebaceous glands and prostate.

• Effect: Promotes a significant increase in lean body mass, bolstering the strength and durability of muscle and bone.

RAD-140 (Testolone) - 5-20mg per Day for 6 Weeks

• Pathway: Unlike other SARMs, RAD-140 shows particular effectiveness in stimulating ARs in the brain, which may protect brain cells.

• Effect: Provides significant anabolic effects, increases muscle mass and burns fat, and offers neuroprotective effects.

YK-11 - 5-15mg per Day for 6 Weeks

• Pathway: YK-11 is believed to inhibit the action of myostatin, which is crucial because myostatin limits muscle growth. By inhibiting myostatin, YK-11 potentially allows for increased muscle mass beyond typical genetic limits.

• Effect: Like other SARMs, YK-11 binds to androgen receptors which can stimulate anabolic activities in muscle and bone tissues.

References

1. Dalton, J. T., Barnette, K. G., Bohl, C. E., Hancock, M. L., Rodriguez, D., Dodson, S. T., Morton, R. A., & Steiner, M. S. (2011). The selective androgen receptor modulator GTx-024 (enobosarm) improves lean body mass and physical function in healthy elderly men and postmenopausal women: Results of a double-blind, placebo-controlled phase II trial. Journal of Cachexia, Sarcopenia and Muscle, 2(3), 153-161.

2. Narayanan, R., Mohler, M. L., Bohl, C. E., Miller, D. D., & Dalton, J. T. (2008). Selective androgen receptor modulators in preclinical and clinical development. Nuclear Receptor Signaling, 6, e010.

3. Basaria, S., Collins, L., Dillon, E. L., Orwoll, K., Storer, T. W., Miciek, R., Ulloor, J., Zhang, A., Eder, R., Zientek, H., Gordon, G., Kazmi, S., Sheffield-Moore, M., & Bhasin, S. (2013). The safety, pharmacokinetics, and effects of LGD-4033, a novel nonsteroidal oral, selective androgen receptor modulator, in healthy young men. Journals of Gerontology Series A: Biological Sciences and Medical Sciences, 68(1), 87-95.

4. Chen, J., Kim, J., Dalton, J. T. (2005). Discovery and therapeutic promise of selective androgen receptor modulators. Molecular Interventions, 5(3), 173-188.

5. Gao, W., & Dalton, J. T. (2007). Ostarine (MK-2866): a potent and selective androgen receptor modulator in clinical development for muscle wasting and functional improvement. Recent Advances in the Development of Anti-Obesity Drugs, 1(1), 59-74.

6. Jones, A., & Chen, J. (2010). Clinical potential of novel selective androgen receptor modulators (SARMs) for the treatment of osteoporosis. Menopause Review/Przegląd Menopauzalny, 9(4), 210-217.

7. Thevis, M., Schänzer, W. (2008). Detection of SARMs in doping control analysis. Molecular Nutrition & Food Research, 52(9), 1106-1114.

8. Bhasin, S., Jasuja, R. (2009). Selective androgen receptor modulators as function promoting therapies. Current Opinion in Clinical Nutrition and Metabolic Care, 12(3), 232-240.

9. Segal, S., Narayanan, R., Dalton, J. T. (2006). Therapeutic potential of the SARMs: Revisiting the androgen receptor for drug discovery. Expert Opinion on Investigational Drugs, 15(4), 377-387.