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Current Trends in Performance- and Image-Enhancing Substance Use Among Gym Goers, Exercisers, and Athletes
Published in Ornella Corazza, Andres Roman-Urrestarazu, Handbook of Novel Psychoactive Substances, 2018
Neha P. Ainsworth, Jake Shelley, Andrea Petróczi
Cardarine (also known as GW501516, and on the black market as ‘endurobol’) is a PPARδ nuclear receptor agonist. PPARδ is one of three PPAR isotypes (along with PPARα and PPARγ) and is expressed in adipose, liver, skin, brain, and skeletal muscle tissue.
Peroxisome proliferator-activated receptor agonists and antagonists: a patent review (2014-present)
Published in Expert Opinion on Therapeutic Patents, 2020
Ichiro Takada, Makoto Makishima
Novel synthetic PPAR ligands were reported to have therapeutic effects in many disease models, such as obesity, atherosclerosis, inflammatory bowel disease, and neuroinflammatory disease, in addition to hyperlipidemia and type 2 diabetes [2]. Although some of these compounds were subjected to clinical trials, adverse effects, specifically carcinogenic effect, prevent their clinical application [107]. The PPARα fibrate ligands have a risk of liver damage in humans, although the peroxisome proliferating effect is specific to rodent liver [108]. Fibrate treatment may also increase the risk of gall stone [109]. The PPARδ agonist GW501516 successfully met endpoints in clinical trials for the treatment of dyslipidemia and type 2 diabetes, however animal experiments raise concern for carcinogenesis [110]. Clinical trials of the PPARγ ligand troglitazone proved its anti-diabetic effect but raised a concern of hepatoxicity [111]. Troglitazone was later withdrawn from the market [48]. Many researchers are struggling to develop PPAR ligands without adverse effect. Since PPARs are involved in many physiological processes, potent ligands can exhibit both desirable and undesirable effects. The underlying molecular mechanisms for function-selective PPAR actions should be elucidated for the development of novel PPAR-targeting drugs. Beneficial effects of developed PPAR ligands were claimed in a specific disease model. Further careful studies are needed to confirm the safety of novel-patented compounds.
Anabolic-androgenic steroids: procurement and administration practices of doping athletes
Published in The Physician and Sportsmedicine, 2019
Julius Fink, Brad Jon Schoenfeld, Anthony C. Hackney, Masahito Matsumoto, Takahiro Maekawa, Koichi Nakazato, Shigeo Horie
Online sellers also are now offering selective androgen receptor modulators (SARMs), which are believed to have similar effects as AAS without the same degree of negative side effects due to their discriminating targeting of receptors. However, steroid-like side effects such as liver toxicity, increased potential of heart attack and stroke, infertility and mental health problems may also occur with the usage of SARMs. The term ‘selective’ in SARM means they preferentially bind to androgen receptors in muscle tissue without triggering androgenic effects in other tissues such as the prostate [13–15]. The popularity of SARMs has also increased among athletes seeking anabolic effects while minimizing androgenic side effects. The legal status of SARMs allows many websites to legally sell these products as ‘research products not for human consumption’. Popular SARMs include Andarine, Accadine (AC-262,536), Cardarine, Endurobol (GW501516), Mk-677 (Ibutamoren), Ligandrol (LGD-4033), Ostarine (Mk-2866), Trestolone (RAD-140), S-23, Stenabolic (SR-9009) and YK-11. Even though not approved by the Food and Drug Administration (FDA), many individuals on the black market take advantage of the fact that SARMs are not yet listed as banned substances and can therefore be sold as research drugs, despite being banned by the World Anti-Doping Agency. Athletes who do not want to procure AAS via illegal routes might buy SARMs without realizing the long-term side effects of these drugs are still under investigation, even though similar side effects to AAS have been observed.
Treatment challenges and delivery systems in immunomodulation and probiotic therapies for periodontitis
Published in Expert Opinion on Drug Delivery, 2021
Anže Zidar, Julijana Kristl, Petra Kocbek, Špela Zupančič
The clearance of apoptotic neutrophils by efferocytosis is very important for the macrophage inflammation-resolving phenotype switch, and so for resolution of periodontal inflammation [12]. Peroxisome proliferator-activated receptor delta (PPARδ), which is expressed in many tissues, stimulates macrophage efferocytosis [55,56]. Systemic injection of a small-molecule PPARδ agonist (GW501516) showed favorable results in a rat model of periodontal disease [57]. On the other hand, age-related changes in immune progenitor cell niches can also be the cause for immune system dysfunction. Systemic application of the small-molecule drug rapamycin has been shown to restore hematopoietic stem cell self-renewal, which can also help resolve leukocyte dysfunction in periodontitis [58,59].