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selective anabolic receptor modulator

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https://www.readbyqxmd.com/read/29727238/treatment-of-osteoporosis-whom-how-and-for-how-long
#1
Anastasia D Dede, Margaret Callan
Identification of patients at risk for fragility fractures is the first important step in the management of osteoporosis. Bisphosphonates have been the mainstay of treatment for decades, whereas denosumab and selective oestrogen receptor modulators are other available licensed antiresorptive drugs. Currently teriparatide is the only approved anabolic agent in Europe, while abaloparatide and romosozumab are awaiting approval and might be available in the near future. For bisphosphonates, current guidance suggests an initial treatment course of 3-5 years and more prolonged treatment should be pursued in patients with higher fracture risk...
May 2, 2018: British Journal of Hospital Medicine
https://www.readbyqxmd.com/read/29704771/new-approach-based-on-immunochemical-techniques-for-monitoring-of-selective-estrogen-receptor-modulators-serms-in-human-urine
#2
J-Pablo Salvador, Ester Vila-Roca, Núria Monfort, Rosa Ventura, M-Pilar Marco
Antiestrogenic compounds such as tamoxifen, toremifen and chlomifen are used illegally by athletes to minimize physical impacts such as gynecomastia resulting from the secondary effects of anabolic androgenic steroids, used to increase athletic efficiency unlawfully. The use of these compounds is banned by the World Anti-Doping Agency (WADA) and controls are made through analytical methodologies such as HPLC-MS/MS, which do not fulfil the sample throughput requirements. Moreover, compounds such as tamoxifen are also used to treat hormone receptor-positive breast cancer (ER + )...
April 22, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29621580/use-of-nutritional-supplements-contaminated-with-banned-doping-substances-by-recreational-adolescent-athletes-in-athens-greece
#3
Konstantinos Tsarouhas, Nassia Kioukia-Fougia, Petros Papalexis, Aristidis Tsatsakis, Dimitrios Kouretas, Flora Bacopoulou, Christina Tsitsimpikou
Although the use of nutritional supplements by adult athletes has been extensively studied, information on supplements consumption by adolescent athletes is still limited. The present study reports on the use of nutritional supplements contaminated with banned doping substances among 170 recreational adolescent athletes from eleven, randomly selected, gym centres, in Athens, Greece. Nutritional supplements consumption was reported by almost 60% of the study population, with proteins/amino acids and vitamins being the most popular...
April 2, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29621030/long-term-treatment-strategies-for-postmenopausal-osteoporosis
#4
Felicia Cosman
PURPOSE OF REVIEW: Osteoporosis guidelines do not usually provide specific recommendations regarding what medication is most appropriate for individual patients. Generic oral bisphosphonates are often considered first-line treatment for osteoporosis, but treatment duration is limited, based on potential long-term safety concerns, and there is no consensus about what to do after 5 years. There are no recommendations concerning long-term management of osteoporosis over 30 or more years of postmenopausal life...
April 4, 2018: Current Opinion in Rheumatology
https://www.readbyqxmd.com/read/29499416/amino-acids-as-signaling-molecules-modulating-bone-turnover
#5
REVIEW
Ke-Hong Ding, Michael Cain, Michael Davis, Clare Bergson, Meghan McGee-Lawrence, Crystal Perkins, Trevor Hardigan, Xingming Shi, Qing Zhong, Jianrui Xu, Wendy B Bollag, William Hill, Mohammed Elsalanty, Monte Hunter, Maria C Isales, Patricia Lopez, Mark Hamrick, Carlos M Isales
Except for the essential amino acids (AAs), much of the focus on adequate dietary protein intake has been on total nitrogen and caloric intake rather than AA composition. Recent data, however, demonstrate that "amino-acid sensing" can occur through either intracellular or extracellular nutrient-sensing mechanisms. In particular, members of the class 3 G-protein coupled receptor family, like the calcium-sensing receptor are known to preferentially bind specific AAs, which then modulate receptor activation by calcium ions and thus potentially impact bone turnover...
February 27, 2018: Bone
https://www.readbyqxmd.com/read/29491216/selective-androgen-receptor-modulator-yk11-up-regulates-osteoblastic-proliferation-and-differentiation-in-mc3t3-e1-cells
#6
Tomofumi Yatsu, Taichi Kusakabe, Keisuke Kato, Yoshio Inouye, Kiyomitsu Nemoto, Yuichiro Kanno
Androgens are key regulators that play a critical role in the male reproductive system and have anabolic effects on bone mineral density and skeletal muscle mass. We have previously reported that YK11 is a novel selective androgen receptor modulator (SARM) and induces myogenic differentiation and selective gene regulation. In this study, we show that treatment of YK11 and dihydrotestosterone (DHT) accelerated cell proliferation and mineralization in MC3T3-E1 mouse osteoblast cells. Further, YK11-treated cells increased osteoblast specific differentiation markers, such as osteoprotegerin and osteocalcin, compared to untreated cells...
2018: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29430877/detection-of-prohibited-substances-in-equine-hair-by-ultra-high-performance-liquid-chromatography-triple-quadrupole-mass-spectrometry-application-to-doping-control-samples
#7
B Gray, M Viljanto, E Menzies, L Vanhaecke
The detection of drugs in human hair samples has been performed by laboratories around the world for many years and the matrix is popular in disciplines, such as workplace drug testing. To date, however, hair has not become a routinely utilised matrix in sports drug detection. The analysis of hair samples offers several potential advantages to doping control laboratories, not least of which are the greatly extended detection window and the ease of sample collection and storage. This article describes the development, validation, and utilisation of a sensitive ultra-high performance liquid chromatography-triple quadrupole mass spectrometry (UHPLC-MS/MS) method for the detection of 50 compounds...
February 12, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29344250/prevention-of-body-weight-loss-and-sarcopenia-by-a-novel-selective-androgen-receptor-modulator-in-cancer-cachexia-models
#8
Megumi Morimoto, Katsuji Aikawa, Takahito Hara, Masuo Yamaoka
Cancer cachexia is a syndrome that impairs the quality of life and overall survival of patients, and thus the effectiveness of anticancer agents. There are no effective therapies for cancer cachexia due to the complexity of the syndrome, and insufficient knowledge of its pathogenesis results in difficulty establishing appropriate animal models. Previously, promising results have been obtained in clinical trials using novel agents including the ghrelin receptor agonist anamorelin, and the selective androgen receptor modulator (SARM) enobosarm to treat cachexia in patients with cancer...
December 2017: Oncology Letters
https://www.readbyqxmd.com/read/29334634/equine-in-vivo-derived-metabolites-of-the-sarm-lgd-4033-and-comparison-with-human-and-fungal-metabolites
#9
Annelie Hansson, Heather Knych, Scott Stanley, Emma Berndtson, Liora Jackson, Ulf Bondesson, Mario Thevis, Mikael Hedeland
LGD-4033 has been found in human doping control samples and has the potential for illicit use in racehorses as well. It belongs to the pharmacological class of selective androgen receptor modulators (SARMs) and can stimulate muscle growth, much like anabolic steroids. However, SARMs have shown superior side effect profiles compared to anabolic steroids, which arguably makes them attractive for use by individuals seeking an unfair advantage over their competitors. The purpose of this study was to investigate the metabolites formed from LGD-4033 in the horse in order to find suitable analytical targets for doping controls...
February 1, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29216311/amelioration-of-sexual-behavior-and-motor-activity-deficits-in-a-castrated-rodent-model-with-a-selective-androgen-receptor-modulator-sarm-2f
#10
Megumi Morimoto, Yuichiro Amano, Masahiro Oka, Ayako Harada, Hisashi Fujita, Yukiko Hikichi, Ryuichi Tozawa, Masuo Yamaoka, Takahito Hara
Sarcopenia and cachexia present characteristic features of a decrease in skeletal muscle mass and strength, anorexia, and lack of motivation. Treatments for these diseases have not yet been established, although selective androgen receptor modulators (SARMs) are considered as therapeutic targets. We previously reported that a novel SARM compound, SARM-2f, exhibits anabolic effect on muscles, with less stimulatory effect on prostate weight compared with testosterone, in rat Hershberger assays and cancer cachexia models...
2017: PloS One
https://www.readbyqxmd.com/read/29120657/-anabolic-steroid-induced-hypogonadism-in-men-overview-and-case-report
#11
Luboslav Stárka, Michaela Dušková, Lucie Kolátorová, Oldřich Lapčík
An important potential consequence of the anabolic steroid misuse is hypogonadotropic hypogonadism due to the inhibition of pituitary secretion of gonadotropins. By the symptoms as testicular atrophy, spermatogenic and fertility disturbances or dysfunction in sexual life, the anabolic steroids induced hypogonadism (ASIH) could be differentiated from organic hypogonadotropic hypogonadism only with difficulty unless the misuse is reported by the user. When diagnosed, the crucial step in the therapy is the stop of anabolic use...
December 0: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/28454849/synthesis-and-biological-evaluation-of-novel-selective-androgen-receptor-modulators-sarms-part-iii-discovery-of-4-5-oxopyrrolidine-1-yl-benzonitrile-derivative-2f-as-a-clinical-candidate
#12
Katsuji Aikawa, Moriteru Asano, Koji Ono, Noriyuki Habuka, Jason Yano, Keith Wilson, Hisashi Fujita, Hitoshi Kandori, Takahito Hara, Megumi Morimoto, Takashi Santou, Masuo Yamaoka, Masaharu Nakayama, Atsushi Hasuoka
We previously reported that 4-(pyrrolidin-1-yl)benzonitrile derivative 1b was a selective androgen receptor modulator (SARM) that exhibited anabolic effects on organs such as muscles and the central nervous system (CNS), but neutral effects on the prostate. From further modification, we identified that 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2a showed strong AR binding affinity with improved metabolic stabilities. Based on these results, we tried to enhance the AR agonistic activities by modifying the substituents of the 5-oxopyrrolidine ring...
July 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28453658/androgen-receptor-agonists-increase-lean-mass-improve-cardiopulmonary-functions-and-extend-survival-in-preclinical-models-of-duchenne-muscular-dystrophy
#13
Suriyan Ponnusamy, Ryan D Sullivan, Dahui You, Nadeem Zafar, Chuan He Yang, Thirumagal Thiyagarajan, Daniel L Johnson, Maron L Barrett, Nikki J Koehler, Mayra Star, Erin J Stephenson, Dave Bridges, Stephania A Cormier, Lawrence M Pfeffer, Ramesh Narayanan
Duchenne muscular dystrophy (DMD) is a neuromuscular disease that predominantly affects boys as a result of mutation(s) in the dystrophin gene. DMD is characterized by musculoskeletal and cardiopulmonary complications, resulting in shorter life-span. Boys afflicted by DMD typically exhibit symptoms within 3-5 years of age and declining physical functions before attaining puberty. We hypothesized that rapidly deteriorating health of pre-pubertal boys with DMD could be due to diminished anabolic actions of androgens in muscle, and that intervention with an androgen receptor (AR) agonist will reverse musculoskeletal complications and extend survival...
July 1, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/28449232/safety-pharmacokinetics-and-pharmacological-effects-of-the-selective-androgen-receptor-modulator-gsk2881078-in-healthy-men-and-postmenopausal-women
#14
Richard V Clark, Ann C Walker, Susan Andrews, Philip Turnbull, Jeffrey A Wald, Mindy H Magee
AIM: Selective androgen receptor modulators (SARMs) induce anabolic effects on muscle without the adverse effects of androgenic steroids. In this first-in-human study, we report the safety, tolerability, pharmacokinetics (PK) and pharmacodynamics of the SARM GSK2881078. METHODS: In Part A, healthy young men (n = 10) received a single dose of study drug (0 mg, 0.05 mg, 0.1 mg, 0.2 mg GSK2881078 or matching-placebo). In Part B, repeat-dose cohorts in men (n = 65) were 0...
October 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28440570/mass-spectrometric-characterization-of-the-selective-androgen-receptor-modulator-sarm-yk-11-for-doping-control-purposes
#15
Mario Thevis, Thomas Piper, Josef Dib, Andreas Lagojda, Dirk Kühne, Lars Packschies, Hans Geyer, Wilhelm Schänzer
RATIONALE: Selective androgen receptor modulators (SARMs) represent an emerging class of therapeutics targeting inter alia conditions referred to as cachexia and sarcopenia. Due to their anabolic properties, the use of SARMs is prohibited in sports as regulated by the World Anti-Doping Agency (WADA), and doping control laboratories test for these anabolic agents in blood and urine. In order to accomplish and maintain comprehensive test methods, the characterization of new drug candidates is critical for efficient sports drug testing...
July 30, 2017: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/28137616/detection-of-sarms-in-doping-control-analysis
#16
Mario Thevis, Wilhelm Schänzer
The class of selective androgen receptor modulators (SARMs) has been the subject of intense and dedicated clinical research over the past two decades. Potential therapeutic applications of SARMs are manifold and focus particularly on the treatment of conditions manifesting in muscle loss such as general sarcopenia, cancer-associated cachexia, muscular dystrophy, etc. Consequently, based on the substantial muscle- and bone-anabolic properties of SARMs, these agents constitute substances with significant potential for misuse in sport and have therefore been added to the Word Anti-Doping Agency's (WADA's) Prohibited List in 2008...
March 15, 2018: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28131133/combined-pharmacologic-therapy-in-postmenopausal-osteoporosis
#17
REVIEW
Yang Shen, Dona L Gray, Dorothy S Martinez
Antiresorptive agents for treating postmenopausal osteoporosis include selective estrogen receptor modulator (SERM), bisphosphonates and denoumab. Teriparatide is the only Food and Drug Administration-approved anabolic agent. Synergistic effects of combining teriparatide with an antiresorptive agent have been proposed and studied. This article reviews the trial designs and the outcomes of combination therapies. Results of the combination therapy for teriparatide and bisphosphonates were mixed; while small increases of bone density were observed in the combination therapy of teriparatide and estrogen/SERM and that of teriparatide and denosumab...
March 2017: Endocrinology and Metabolism Clinics of North America
https://www.readbyqxmd.com/read/28054434/in-vitro-phase-i-metabolism-of-selective-estrogen-receptor-modulators-in-horse-using-ultra-high-performance-liquid-chromatography-high-resolution-mass-spectrometry
#18
Karen Y Kwok, George H M Chan, Wai Him Kwok, Jenny K Y Wong, Terence S M Wan
Selective estrogen receptor modulators (SERMs) are chemicals that possess the anti-oestrogenic activities that are banned 'in' and 'out' of competition by the World Anti-Doping Agency (WADA) in human sports, and by the International Federation of Horseracing Authorities (IFHA) in horseracing. SERMs can be used as performance-enhancing drugs to boost the level of androgens or to compensate for the adverse effects as a result of extensive use of androgenic anabolic steroids (AASs). SERMs have indeed been abused in human sports; hence, a similar threat can be envisaged in horseracing...
September 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28030966/systemic-drugs-that-influence-titanium-implant-osseointegration
#19
REVIEW
Dragos Apostu, Ondine Lucaciu, Gheorghe Dan Osvald Lucaciu, Bogdan Crisan, Liana Crisan, Mihaela Baciut, Florin Onisor, Grigore Baciut, Radu Septimiu Câmpian, Simion Bran
Titanium implants are widely used on an increasing number of patients in orthopedic and dental medicine. Despite the good survival rates of these implants, failures that lead to important socio-economic consequences still exist. Recently, research aimed at improving implant fixation, a process called osseointegration, has focused on a new, innovative field: systemic delivery of drugs. Following implant fixation, patients receive systemic drugs that could either impair or enhance osseointegration; these drugs include anabolic and anti-catabolic bone-acting agents in addition to new treatments...
February 2017: Drug Metabolism Reviews
https://www.readbyqxmd.com/read/28008373/clinical-factors-disease-parameters-and-molecular-therapies-affecting-osseointegration-of-orthopedic-implants
#20
Hilal Maradit Kremers, Eric A Lewallen, Andre J van Wijnen, David G Lewallen
Total hip and knee arthroplasty are effective interventions for management of end-stage arthritis. Indeed, about 7 million Americans are currently living with artificial hip and knee joints. The majority of these individuals, however, will outlive their implants and require revision surgeries, mostly due to poor implant osseointegration and aseptic loosening. Revisions are potentially avoidable with better management of patient-related risk factors that affect the osseointegration of orthopedic implants. In this review, we summarize the published clinical literature on the role of demographics, biologic factors, comorbidities, medications and aseptic loosening risk...
September 2016: Current Molecular Biology Reports
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