What are selective androgen receptor modulators (SARMs) & why do bodybuilders use them? | Derek MPMD

Summary

This conversation explores SARMs (Selective Androgen Receptor Modulators), comparing them with selective estrogen receptor modulators (SERMs) and anabolic steroids. It delves into their unique ability to target specific tissues for muscle building with minimal androgenic effects. The discussion covers common SARMs like LGD-4033 and Ostarine, their use in bodybuilding, and their detection in natural bodybuilding. The conversation also touches on other compounds such as Tren, Deca, and Testosterone, highlighting their anabolic properties, side effects, and roles in muscle development. The complexities of their mechanisms are thoroughly explored, giving insight into their benefits and risks.

Takeaways

• 😀 SARMs (Selective Androgen Receptor Modulators) are compounds designed to interact with androgen receptors in a tissue-specific manner, aiming for anabolic effects with minimal androgenic side effects.
• 😀 SARMs are similar to selective estrogen receptor modulators (SERMs), which target estrogen receptors in specific tissues, offering benefits such as inhibiting breast cancer while promoting bone health.
• 😀 While SARMs are generally more selective and potentially less harmful than anabolic steroids, their muscle-building effects are less potent, requiring higher doses for more significant results.
• 😀 Common SARMs include LGD-4033 (Ligandrol), Ostarine (Enobosarm), and VK5211, with applications ranging from bodybuilding to treating bone fractures.
• 😀 Ostarine (Enobosarm) is one of the most well-known SARMs, though it has not been FDA-approved for clinical use and has failed to meet certain trial endpoints.
• 😀 SARMs are banned in natural bodybuilding due to their detectable presence in the body, and athletes can obtain them through underground labs or compounding pharmacies.
• 😀 Trenbolone, although classified as a steroidal SARM, was used in the '80s for both human and veterinary purposes. It is highly anabolic but has notable side effects such as night sweats (Tren sweats) and severe coughing (Tren cough).
• 😀 Trenbolone interacts with progesterone receptors, which adds to its side effects and increases the likelihood of negative feedback from both androgen and progesterone receptors.
• 😀 Nandrolone, a commonly used anabolic steroid (Deca), can help build muscle without causing hair loss due to its unique interaction with 5-alpha reductase, resulting in different metabolite effects in the muscle and scalp.
• 😀 Despite the availability of designer anabolic compounds, testosterone is still commonly used by bodybuilders as it provides a stable base for estrogen conversion, neuroprotection, and balanced androgenic activity.

Q & A

What are SARMs and how do they function in the body?

SARMs, or Selective Androgen Receptor Modulators, are compounds designed to interact with androgen receptors in a tissue-specific way, aiming to promote anabolic effects (muscle-building) while minimizing androgenic effects (like hair loss). They work similarly to selective estrogen receptor modulators (SERMs), which are used for breast cancer treatment by targeting estrogen receptors in different tissues.

How do SARMs differ from anabolic steroids?

While SARMs also promote muscle growth, they are designed to be more selective in their action, targeting specific tissues like muscle and bone, without affecting others. However, the anabolic effect of SARMs is generally weaker than that of anabolic steroids, which can lead to greater muscle gain but also more side effects.

Why might higher doses of SARMs become less selective?

As the dose of SARMs increases, they tend to lose their tissue-specific effects, becoming less selective. This can result in a broader spectrum of action, which might lead to unwanted side effects, much like what happens with other compounds, such as beta blockers.

What are some of the most commonly used SARMs?

Some of the most commonly used SARMs include LGD-4033 (Ligandrol), Ostarine (Enobosarm), and VK5211. These compounds are often studied for their potential to treat conditions like muscle wasting and osteoporosis, but they are not FDA-approved.

How are SARMs typically acquired by users?

SARMs are often obtained through underground channels, including compounding pharmacies, which are not regulated. These compounds are usually not available through legal, prescribed means.

What is Tren and how is it classified?

Tren, short for Trenbolone, is classified as a steroidal SARM. Initially prescribed to women in the 1980s, it has potent anabolic properties but also significant side effects, including progesterone receptor interaction, which causes symptoms like night sweats and 'Tren cough'.

What are the main side effects associated with Tren?

Tren is known for causing night sweats (often called 'Tren sweats') and a severe coughing fit, referred to as 'Tren cough', which occurs shortly after injection. These side effects are likely due to its interaction with the progesterone receptor.

How does Deca-Durabolin (Nandrolone) differ from other steroids?

Deca-Durabolin, or Nandrolone, is an anabolic steroid that has a unique property: it reduces into a metabolite that has little androgenic activity, which results in muscle-building effects without hair loss, unlike other steroids that typically cause hair loss due to androgenic activity.

Why do bodybuilders still use testosterone despite the availability of other anabolics?

Testosterone is considered the base for anabolic steroid cycles because it provides a balanced layer of estrogen, which is important for neuroprotection and overall health. Other compounds may have less predictable effects on estrogen and androgen levels, which can lead to imbalances and negative health outcomes.

What happens when hormone levels exceed physiological levels in the body?

When hormone levels exceed physiological levels, particularly through the use of synthetic compounds like SARMs or steroids, it can cause neurotoxic effects and negative feedback on the body's hormonal systems. For example, while synthetic estrogens or high doses of testosterone may provide temporary benefits, they can lead to long-term health issues if the balance is disrupted.