The progress of research into SARM’s (selective androgen receptor modulators which are studied to see the anabolic effects on the muscle/s, however, limited, or at least nominal adverse effects on prostate and cardiovasucular tissues, has taken up considerable interest for the treatment of aging men and women with inadequate endogenous testosterone levels.
Nonsteroidal selective androgen receptor modulators [SARM’s] deviate from testosterone essentially because of their incapability to transform into active metabolites, such as E2 and DHT – while preserving the strength to act as agonists in bone and muscle, yet, only partial agonists in reproductive organs. Additionally, the favorable pharmacodynamics and AR specifics of nonsteroidal selective androgen receptor modulators (SARM’s) correlated to exogenous testosterone enables more precise pharmacological cooperations that serve specific implications for clinical use.
The natural tissue selectivity of SARM’s as gene expression modulators is due to isoform-specific conformational variations, modulation of surface topology, and discrete protein interactions between AR and additional nuclear receptors. Since isoform and ligand-specific receptor conformation and protein complements differ in each tissue, this sequentially drives distinct gene expression.
Nevertheless, not all selective androgen receptor modulators [SARM’s] are being examined for muscle associated phenotypes, are actively being analyzed in the context of prostate cancer and benign prostate hyperplasia. Other SARM’s which have been shown to stimulate gonadotropin suppression only without prostate stimulation might find utilization for aid in male contraception.