selective anabolic receptor modulator

BACKGROUND: Few studies have assessed the use of dietary supplements, anabolic androgenic steroids (AAS) and selective androgen receptor modulators (SARM) in male gym users. The comparison of physical appearance with others on social media and the exposure to fitness-related content on social media (i.e., image-centric social media use) may have a profound role in using these compounds due to its role in creating negative body images in male gym users. OBJECTIVE: Provide contemporary data on the use of dietary supplements, AAS and SARM among young male gym users, and test the hypothesis that social media is associated with the use of dietary supplements, AAS and SARM, as a result of a negative body image...

Selective androgen receptor modulators (SARMs) are a class of drugs presenting identical anabolic properties to anabolic steroids in addition to marked reduced androgenic effects. These drugs have emerged in the doping area within the early 2000's. Ligandrol, ostarine, RAD-140 and andarine are the most popular agents belonging to this class. According to the world anti-doping agency (WADA) prohibited list, SARMs are prohibited at all times (i.e. in and out-of-competition) and are listed under the section S1...

Selective androgen receptor modulators, SARMs, are a large class of compounds developed to provide therapeutic anabolic effects with minimal androgenic side effects. A wide range of these compounds are available to purchase online, and thus provide the potential for abuse in sports. Knowledge of the metabolism of these compounds is essential to aid their detection in doping control samples. In vitro models allow a quick, cost-effective response where administration studies are yet to be carried out. In this study, the equine phase I metabolism of the non-steroidal SARMs GSK2881078, LGD-2226, LGD-3303, PF-06260414, ACP-105, RAD-140 and S-23 was investigated using equine liver microsomes...

To characterise trends and interest in selective androgen receptor modulators (SARMs). SARMs are androgen receptor ligands that bind androgen receptors selectively. SARMs have anabolic effects on muscle and bone and were originally synthesised for treatment of muscle wasting conditions, osteoporosis and breast cancer. To date, no SARM has been clinically approved and little is known about their beneficial effects and other adverse effects on users. We examined Google Trend searches of SARMs. Using Google Trends, we analysed how interest in SARMs has evolved over the last 15 years and compared it to trends in testosterone...

Selective androgen receptor modulators (SARMs) are a class of androgen receptor ligands that bind androgen receptors and display tissue selective activation of androgenic signaling. SARMs have selective anabolic effects on muscle and bone, and were originally synthesized for treatment of muscle wasting conditions, osteoporosis, breast cancer. To date, no SARM has been clinically approved and little is known about the beneficial effects and other adverse effects on users. We examined the adverse effects and potential benefits of SARMs amongst users...

Osteoporosis is a common chronic condition that markedly increases the risk of fractures. Osteoporotic-related fractures increase morbidity and mortality and impair quality of life. Therefore, a correct approach for fracture prevention seems mandatory. Lifestyle changes should be recommended to all patients, including weight reduction if patients are obese/overweight, increasing physical activity and avoiding alcohol consumption and smoking. Additionally, calcium and vitamin D3 should be prescribed until the vitamin D deficit is resolved...

The pressure to gain mass, power, explosiveness, and endurance and to obtain a performance edge continues to a part of sports. Anabolic agents, including selective androgen receptor modulators along with peptides, hormones, and metabolic modulators, continues to evolve. Methods to promote transcription to modify gene expression are a part of the evolution. In order to monitor and improve doping detection, the Athlete Biological Passport has been created. This article provides an up-to-date review of alcohol, anabolic androgens and related agents, stimulants, opioids, and cannabis and related compounds and their effects on athlete health and performance...

Anabolic steroids are well-known to cause liver injury, which may manifest with jaundice and elevated liver enzymes. Selective androgen receptor modulators (SARMs) have been developed to enhance muscle bulk without the side effects associated with exogenous androgen steroids. We report a case of significant cholestatic liver injury associated with a SARM, ostarine (enobosarm), similar to that associated with anabolic steroids. Liver injury from SARMs has not been reported frequently, and we speculate that this may be seen more often as the consumption of SARMs increases in the athletic market...

On the cellular level, osteoporosis (OP) is a result of imbalanced bone remodeling, in which osteoclastic bone resorption outcompetes osteoblastic bone formation. Currently available OP medications include both antiresorptive and bone-forming drugs. However, their long-term use in OP patients, mainly in postmenopausal women, is accompanied by severe side effects. Notably, the fundamental coupling between bone resorption and formation processes underlies the existence of an undesirable secondary outcome that bone anabolic or anti-resorptive drugs also reduce bone formation...

Performance- and image-enhancing drug (PIED) misuse is a significant public health issue. Currently, seizure data, surveys, anti-doping testing, and needle service provider data are used to estimate PIED use in populations. These methods are time consuming, single point-in-time measurements that often consist of small sample sizes and do not truly capture PIED prevalence. Wastewater-based epidemiology (WBE) has been used globally to assess and monitor licit and illicit drug consumption within the general community...

BACKGROUND: Muscle growth promoters are being developed for the treatment of disease-induced loss of muscle mass. Ligandrol and ostarine are selective androgen receptor modulators (SARMs) with a non-steroidal structure and a presumably more favorable side effect profile. In recent years, these substances with or without "post-cycle therapy" (PCT) are often misused by amateur athletes aiming to promote muscle growth. At the same time, reports on their toxic effects on organ systems are emerging...

Introduction : Anabolic androgenic steroid use is an uncommon but important cause of male infertility. As paternal age and anabolic steroid use increases, providers are more likely than ever to encounter men with infertility and prior or concurrent anabolic steroid use. In this review, we outline the background, epidemiology and pathophysiology of anabolic steroid induced male infertility and provide recommendations regarding the diagnosis, management, and future prevention of this condition. Areas covered : Male reproductive physiology is a tightly regulated process that can be influenced by exogenous sources such as anabolic steroids and selective androgen receptor modulators (SARMs)...

Androgens, both steroidal and non-steroidal in nature, are among the most commonly misused substances in competitive sports. Their recognized anabolic and performance enhancing effects through short- and long-term physiological adaptations make them popular. Androgens exist as natural steroids, or are chemically synthesized as anabolic androgenic steroids (AAS) or selective androgen receptor modulators (SARMs). In order to effectively detect misuse of androgens, targeted strategies are used. These targeted strategies rely heavily on mass spectrometry and detection requires prior knowledge of the targeted structure and its metabolites...

CASE: A 36-year-old male competitive powerlifter sustained asynchronous bilateral Achilles tendon ruptures after using 2 types of selective androgen receptor modulators (SARMs). Both tendon ruptures occurred near the myotendinous junction and were treated with open surgical repair and an initial period of immobilization followed by progressive weightbearing and rehabilitation; no postoperative complications were observed. CONCLUSION: Previous studies have reported that anabolic androgenic steroids have a deleterious impact on tendon structure and function...

Use of the selective estrogen receptor modulator Tamoxifen (TAM) is a mainstay to induce conditional expression of Cre recombinase in transgenic laboratory mice. To excise β-catenin fl/fl in 28-day-old male and female Prrx1-CreER/β-catenin fl/fl mice (C57BL/6), we utilized TAM at 150 mg/kg; despite β-catenin knockout in MSC, we found a significant increase in trabecular and cortical bone volume in all genders. Because TAM was similarly anabolic in KO and control mice, we investigated a dose effect on bone formation by treating wild-type mice (WT C57BL/6, 4 weeks) with TAM (total dose 0, 20, 40, 200 mg/kg via four injections)...

Testosterone derivatives and related compounds (such as anabolic-androgenic steroids-AAS) are frequently misused by athletes (both professional and amateur) wishing to promote muscle development and strength or to cover AAS misuse. Even though these agents are vastly regarded as abusive material, they have important pharmacological activities that cannot be easily replaced by other drugs and have therapeutic potential in a range of conditions (e.g., wasting syndromes, severe burns, muscle and bone injuries, anemia, hereditary angioedema)...

Pubertal male Syrian hamsters (Mesocricetus auratus) treated with anabolic/androgenic steroids (AASs) during adolescence (P27-P56) display a highly intense aggressive phenotype that shares many behavioral similarities with pathological aggression in youth. Anticonvulsant drugs like valproate that enhance the activity of the γ-aminobutyric acid (GABA) neural system in the brain have recently gained acceptance as a primary treatment for pathological aggression. This study examined whether valproate would selectively suppress adolescent AAS-induced aggressive behavior and whether GABA neural signaling through GABAA subtype receptors in the latero-anterior hypothalamus (LAH; an area of convergence for developmental and neuroplastic changes that underlie aggression in hamsters) modulate the aggression-suppressing effect of this anticonvulsant medication...

The temporal dynamics of calcium signaling are critical regulators of chondrocyte homeostasis and chondrogenesis. Calcium oscillations regulate differentiation and anabolic processes in chondrocytes and their precursors. Attempts to control chondrocyte calcium signaling have been achieved through mechanical perturbations and synthetic ion channel modulators. However, such stimuli can lack both local and global specificity and precision when evoking calcium signals. Synthetic signaling platforms can more precisely and selectively activate calcium signaling, enabling improved dissection of the roles of intracellular calcium ([Ca2+ ]i ) in chondrocyte behavior...

Selective Androgen Receptor Modulators (SARMs) have anabolic properties but less adverse effects than anabolic androgenic steroids. They are prohibited in both equine and human sports and there have been several cases of SARMs findings reported over the last few years. The aim of this study was to investigate the metabolite profile of the SARM ACP-105 (2-chloro-4-[(3-endo)-3-hydroxy-3-methyl-8-azabicyclo[3.2.1]oct-8-yl]-3-methylbenzonitrile) in order to find analytical targets for doping control. Oral administration of ACP-105 was performed in horses, where blood and urine samples were collected over a time period of 96 h...

Glucocorticoids display remarkable anti-inflammatory activity, but their use is limited by on-target adverse effects including insulin resistance and skeletal muscle atrophy. We used a chemical systems biology approach, ligand class analysis, to examine ligands designed to modulate glucocorticoid receptor activity through distinct structural mechanisms. These ligands displayed diverse activity profiles, providing the variance required to identify target genes and coregulator interactions that were highly predictive of their effects on myocyte glucose disposal and protein balance...