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selective anabolic receptor modulator

Dante Rojas, Gaud Dervilly-Pinel, Nora Cesbron, Mylène Penot, Alexandre Sydor, Stéphanie Prévost, Bruno Le Bizec
Besides their development for therapeutic purposes, non-steroidal selective androgen receptor modulators (non-steroidal SARMs) are also known to impact growth associated pathways as ligands of androgenic receptors (AR). They present thus a potential for abuse in sports and food producing animals as an interesting alternative to anabolic androgenic steroids (AAS). These compounds are easily available and could therefore be (mis)used in livestock production as growth promoters. To prevent such practices, dedicated analytical strategies have to be developed for specific and sensitive detection of these compounds in biological matrices...
October 11, 2016: Drug Testing and Analysis
Christian Görgens, Sven Guddat, Andreas Thomas, Philipp Wachsmuth, Anne-Katrin Orlovius, Gerd Sigmund, Mario Thevis, Wilhelm Schänzer
So far, in sports drug testing compounds of different classes are processed and measured using different screening procedures. The constantly increasing number of samples in doping analysis, as well as the large number of substances with doping related, pharmacological effects require the development of even more powerful assays than those already employed in sports drug testing, indispensably with reduced sample preparation procedures. The analysis of native urine samples after direct injection provides a promising analytical approach, which thereby possesses a broad applicability to many different compounds and their metabolites, without a time-consuming sample preparation...
November 30, 2016: Journal of Pharmaceutical and Biomedical Analysis
Suriyan Ponnusamy, Ryan D Sullivan, Thirumagal Thiyagarajan, Heather Tillmann, Robert H Getzenberg, Ramesh Narayanan
OBJECTIVES: To evaluate two selective androgen receptor modulators (SARMs) (GTx-024 and GTx-027) in a post-menopausal animal model in order to determine their effect on pelvic floor muscles. Stress urinary incontinence (SUI), a prevalent condition, is represented by an involuntary leakage of urine that results, at least in part, from weakened or damaged pelvic floor muscles and is triggered by physical stress. Current treatment options are limited with no oral therapies available. The pelvic floor is rich in androgen receptor and molecules with anabolic activity including (SARMs) may serve as therapeutic options for individuals with SUI...
September 28, 2016: Journal of Cellular Biochemistry
Christopher Wu, Jason R Kovac
There has recently been renewed interest in novel clinical applications of the anabolic-androgenic steroid (AAS) testosterone and its synthetic derivatives, particularly given with the rising popularity of testosterone supplementation therapy (TST) for the treatment of male hypogonadism. In this manuscript, we provide a brief review of the history of AAS and discuss clinical applications of two of the more well-known AAS: nandrolone and oxandrolone. Both agents exhibit favorable myotrophic/androgenic ratios and have been investigated for effectiveness in numerous disease states...
October 2016: Current Urology Reports
Frances Milat, Peter R Ebeling
Osteoporosis affects 1.2 million Australians and, in 2012, fractures due to osteoporosis and osteopenia in Australians aged over 50 years cost $2.75 billion. Even minor minimal trauma fractures are associated with increased morbidity and mortality. Despite increasing therapeutic options for managing osteoporosis, fewer than 20% of patients with a minimal trauma fracture are treated or investigated for osteoporosis, so under-treatment is extremely common. Fracture risk assessment is important for selecting patients who require specific anti-osteoporosis therapy...
August 15, 2016: Medical Journal of Australia
Andreas Lagojda, Dirk Kuehne, Oliver Krug, Andreas Thomas, Tina Wigger, Uwe Karst, Wilhelm Schänzer, Mario Thevis
Research into developing anabolic agents for various therapeutic purposes has been pursued for decades. As the clinical utility of anabolic-androgenic steroids has been found to be limited because of their lack of tissue selectivity and associated off-target effects, alternative drug entities have been designed and are commonly referred to as selective androgen receptor modulators (SARMs). While most of these SARMs are of nonsteroidal structure, the drug candidate MK-0773 comprises a 4-aza-steroidal nucleus...
2016: European Journal of Mass Spectrometry
Toshihiko Yanase
In recent years, the drugs, which show anabolic, effect on bone and muscle without stimulating prostate has been developed. They show tissue-specific selective androgen actions and called selective androgen receptor modulators(SARMs). The development of drug targeting bone and muscle in male is very promising as a treatment tool for osteoporosis and sarcopenia in the near future. The clinical study is under going especially in the field of cachexia associated with cancer, but unfortunately there is no drug in the current market at present...
July 2016: Clinical Calcium
Jeffrey Crawford, Carla M M Prado, Mary Ann Johnston, Richard J Gralla, Ryan P Taylor, Michael L Hancock, James T Dalton
Muscle wasting in cancer is a common and often occult condition that can occur prior to overt signs of weight loss and before a clinical diagnosis of cachexia can be made. Muscle wasting in cancer is an important and independent predictor of progressive functional impairment, decreased quality of life, and increased mortality. Although several therapeutic agents are currently in development for the treatment of muscle wasting or cachexia in cancer, the majority of these agents do not directly inhibit muscle loss...
June 2016: Current Oncology Reports
Michael J Chisamore, Michael A Gentile, Gregory Michael Dillon, Matthew Baran, Carlo Gambone, Sean Riley, Azriel Schmidt, Osvaldo Flores, Hilary Wilkinson, Stephen E Alves
The androgen receptor (AR) is a member of the nuclear hormone receptor super family of transcription factors. Androgens play an essential role in the development, growth, and maintenance of male sex organs, as well as the musculoskeletal and central nervous systems. Yet with advancing age, androgens can drive the onset of prostate cancer, the second leading cause of cancer death in males within the United States. Androgen deprivation therapy (ADT) by pharmacologic and/or surgical castration induces apoptosis of prostate cells and subsequent shrinkage of the prostate and prostate tumors...
October 2016: Journal of Steroid Biochemistry and Molecular Biology
Michał Rabijewski
In past few years we observed the increasing of population of men, who are treated with testosterone due to hypogonadism associated with aging but the most of them have no indications to testosterone replacement therapy. The classical symptoms of hypogonadism including depression, loss of libido, erectile dysfunction, and fatigue may be related to any others diseases. The increase in prevalence of androgenic anabolic steroids specifically among younger athletes is also observed. Exogenous testosterone and anabolic androgenic steroids can inhibit the hypothalamic-pituitary-gonadal axis leading to decreasing of endogenous testosterone synthesis and impaired spermatogenesis...
March 2016: Polski Merkuriusz Lekarski: Organ Polskiego Towarzystwa Lekarskiego
Laure Beucher, Gaud Dervilly-Pinel, Nora Cesbron, Mylène Penot, Audrey Gicquiau, Fabrice Monteau, Bruno Le Bizec
Currently under development for therapeutic purposes in human medicine, non-steroidal selective androgen receptor modulators (non-steroidal SARMs) are also known to impact growth associated pathways. As such, they present a potential for abuse in sports and food-producing animals as interesting alternative anabolic substances. Forbidden since 2008 by the World Anti-Doping Agency (WADA) these compounds are however easily available and could be (mis)used in livestock production as growth promoters. To prevent such practices, dedicated analytical strategies have to be developed for specific and sensitive detection of these compounds in biological matrices...
March 16, 2016: Drug Testing and Analysis
Erik Fink Eriksen, Jacques P Brown
Osteoanabolic therapy with parathyroid hormone (PTH(1-84)) or the PTH analogues teriparatide (PTH(1-34), TPTD) and abaloparatide induces a positive remodeling balance and increases modeling and remodeling activity on bone surfaces. As the anabolic action of PTH is primarily remodeling based increased bone turnover maximizes bone accrual. Increased remodeling, however, also increases cortical porosity and reduces mineralization of newly formed bone, which may cause initial reductions in BMD, particularly at sites rich in cortical bone...
May 2016: Bone
J Abram McBride, Robert M Coward
The use of testosterone replacement therapy (TRT) for hypogonadism continues to rise, particularly in younger men who may wish to remain fertile. Concurrently, awareness of a more pervasive use of anabolic-androgenic steroids (AAS) within the general population has been appreciated. Both TRT and AAS can suppress the hypothalamic-pituitary-gonadal (HPG) axis resulting in diminution of spermatogenesis. Therefore, it is important that clinicians recognize previous TRT or AAS use in patients presenting for infertility treatment...
May 2016: Asian Journal of Andrology
Florence Gondret, Annie Vincent, Magalie Houée-Bigot, Anne Siegel, Sandrine Lagarrigue, Isabelle Louveau, David Causeur
BACKGROUND: Changing the energy and nutrient source for growing animals may be an effective way of limiting adipose tissue expansion, a response which may depend on the genetic background of the animals. This study aims to describe the transcriptional modulations present in the adipose tissues of two pig lines divergently selected for residual feed intake which were either fed a high-fat high-fiber (HF) diet or an isocaloric low-fat high-starch diet (LF). RESULTS: Transcriptomic analysis using a porcine microarray was performed on 48 pigs (n = 12 per diet and per line) in both perirenal (PRAT) and subcutaneous (SCAT) adipose tissues...
2016: BMC Genomics
Timothy E Albertson, James A Chenoweth, Daniel K Colby, Mark E Sutter
Awareness of the prevalence of the use of appearance- and performance-enhancing drugs (APEDs) is increasing. Users range from professional athletes and bodybuilders to amateurs and adolescents. Anabolic androgenic steroids (AASs) are the most widely used APEDs, typically for purposes of building muscle mass, in forms that include pills, injections, topical preparations, and transdermal systems. AASs are often used in combination with augmenting drugs taken to enhance androgen production and, for men, to decrease estrogen production...
February 2016: FP Essentials
Mahalakshmi Shankaran, Todd W Shearer, Stephen A Stimpson, Scott M Turner, Chelsea King, Po-Yin Anne Wong, Ying Shen, Philip S Turnbull, Fritz Kramer, Lisa Clifton, Alan Russell, Marc K Hellerstein, William J Evans
Biomarkers of muscle protein synthesis rate could provide early data demonstrating anabolic efficacy for treating muscle-wasting conditions. Androgenic therapies have been shown to increase muscle mass primarily by increasing the rate of muscle protein synthesis. We hypothesized that the synthesis rate of large numbers of individual muscle proteins could serve as early response biomarkers and potentially treatment-specific signaling for predicting the effect of anabolic treatments on muscle mass. Utilizing selective androgen receptor modulator (SARM) treatment in the ovariectomized (OVX) rat, we applied an unbiased, dynamic proteomics approach to measure the fractional synthesis rates (FSR) of 167-201 individual skeletal muscle proteins in triceps, EDL, and soleus...
March 15, 2016: American Journal of Physiology. Endocrinology and Metabolism
Ashraf Saeed, Grant M Vaught, Kostas Gavardinas, Donald Matthews, Jonathan E Green, Pablo Garcia Losada, Heather A Bullock, Nathan A Calvert, Nita J Patel, Stephanie A Sweetana, Venkatesh Krishnan, Judith W Henck, John G Luz, Yong Wang, Prabhakar Jadhav
A transdermal SARM has a potential to have therapeutic benefit through anabolic activity in muscle while sparing undesired effects of benign prostate hyperplasia (BPH) and liver-mediated decrease in HDL-C. 2-Chloro-4-[(2-hydroxy-2-methyl-cyclopentyl)amino]-3-methyl-benzonitrile 6 showed the desired muscle and prostate effects in a preclinical ORX rat model. Compound 6 had minimal effect on HDL-C levels in cynomolgus monkeys and showed human cadaver skin permeability, thus making it an effective tool for proof-of-concept studies in a clinical setting...
January 28, 2016: Journal of Medicinal Chemistry
Henry Todd, Gabriel L Galea, Lee B Meakin, Peter J Delisser, Lance E Lanyon, Sara H Windahl, Joanna S Price
Genome Wide Association Studies suggest that Wnt16 is an important contributor to the mechanisms controlling bone mineral density, cortical thickness, bone strength and ultimately fracture risk. Wnt16 acts on osteoblasts and osteoclasts and, in cortical bone, is predominantly derived from osteoblasts. This led us to hypothesize that low bone mass would be associated with low levels of Wnt16 expression and that Wnt16 expression would be increased by anabolic factors, including mechanical loading. We therefore investigated Wnt16 expression in the context of ageing, mechanical loading and unloading, estrogen deficiency and replacement, and estrogen receptor α (ERα) depletion...
2015: PloS One
Seul Min Choi, Byung-Mu Lee
INTRODUCTION: Anabolic androgenic steroids (AASs) have been in use for decades for the treatment of short stature, severe burns, HIV wasting syndrome, osteoporosis, and anemia. However, their lack of selective effects on certain symptoms and unfavorable pharmacokinetic properties has limited their long-term usage in clinics. AREAS COVERED: Selective androgen receptor modulators (SARMs) have some advantages over AASs; they are highly specific for androgen receptors, are orally available, and, most importantly, act as strong receptor agonists in skeletal muscle and bone, and as weak agonists or antagonists in androgen-responsive tissues such as the prostate and sebaceous glands...
2015: Expert Opinion on Drug Safety
Vanessa Dubois, Ioannis Simitsidellis, Michaël R Laurent, Ferran Jardi, Philippa T K Saunders, Dirk Vanderschueren, Frank Claessens
Androgens increase skeletal muscle mass, but their clinical use is hampered by a lack of tissue selectivity and subsequent side effects. Selective androgen receptor modulators elicit muscle-anabolic effects while only sparingly affecting reproductive tissues. The selective androgen receptor modulator, GTx-024 (enobosarm), is being investigated for cancer cachexia, sarcopenia, and muscle wasting diseases. Here we investigate the role of muscle androgen receptor (AR) in the anabolic effect of GTx-024. In mice lacking AR in the satellite cell lineage (satARKO), the weight of the androgen-sensitive levator ani muscle was lower but was decreased further upon orchidectomy...
December 2015: Endocrinology
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