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Deciphering the selective androgen receptor modulators paradigm

, PhD & , PhD
Pages 191-218 | Published online: 12 Dec 2012

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Ji Hyun Lee, Ji Hye Han, Eun-Ju Jung, Hari Krishna Nallapaneni, Nam Sook Kim, Hyungil Kim, Jongkook Lee & Sun Young Baek. (2021) Development and validation of liquid chromatography-tandem mass spectrometry method for screening six selective androgen receptor modulators in dietary supplements. Food Additives & Contaminants: Part A 38:7, pages 1075-1086.
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Shinya Fujii & Hiroyuki Kagechika. (2019) Androgen receptor modulators: a review of recent patents and reports (2012-2018). Expert Opinion on Therapeutic Patents 29:6, pages 439-453.
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Mamoun Ahram, Ebtihal Mustafa, Shatha Abu Hammad, Mariam Alhudhud, Randa Bawadi, Lubna Tahtamouni, Faisal Khatib & Malek Zihlif. (2018) The cellular and molecular effects of the androgen receptor agonist, Cl-4AS-1, on breast cancer cells. Endocrine Research 43:3, pages 203-214.
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Melissa D. McCradden & Michael D. Cusimano. (2018) Optimized or Hijacked? The Moral Boundaries of Natural Athletic Performance. The American Journal of Bioethics 18:6, pages 26-28.
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Aydogan Aydogdu & Ronald S. Swerdloff. (2016) Emerging medication for the treatment of male hypogonadism. Expert Opinion on Emerging Drugs 21:3, pages 255-266.
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Seul Min Choi & Byung-Mu Lee. (2015) Comparative safety evaluation of selective androgen receptor modulators and anabolic androgenic steroids. Expert Opinion on Drug Safety 14:11, pages 1773-1785.
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Emeka Udedibia & Jed Kaminetsky. (2014) Phase II drugs currently being investigated for the treatment of hypogonadism. Expert Opinion on Investigational Drugs 23:12, pages 1605-1618.
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Articles from other publishers (39)

Emilie Feisthauer, Laurie Gheddar, Jean-Sebastien Raul & Pascal Kintz. (2023) Contamination de compléments alimentaires utilisés par des athlètes. Toxicologie Analytique et Clinique.
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Tajudheen K. Karatt, M. Anwar Sathiq, Saraswathy Laya, Abdul Khader Karakka Kal, Michael Benedict Subhahar, M. P. Muhammed Ajeebsanu, Moses Philip, Marina Rodriguez Caveney & Fatma Mohammed Graiban. (2023) In‐depth metabolic study of nonsteroidal selective androgen receptor modulator GSK2881078 in thoroughbred horses and horse liver microsomes for doping control. Drug Testing and Analysis 15:7, pages 757-768.
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Tajudheen K. Karatt, M. Anwar Sathiq, Saraswathy Laya, Moses Philip, Abdul Khader Karakka Kal & Michael Benedict Subhahar. (2023) Investigation of in vitro generated metabolites of GLPG0492 using equine liver microsomes for doping control. Drug Testing and Analysis 15:6, pages 605-628.
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Tajudheen K. Karatt, M. Anwar Sathiq, Saraswathy Laya, Abdul Khader Karakka Kal, Michael Benedict Subhahar, Muhammed Ajeebsanu M.P, Moses Philip, Fatma Mohammed Graiban & Marina Rodriguez Caveney. (2023) Metabolic study of selective androgen receptor modulator LY2452473 in thoroughbred horses for doping control. Rapid Communications in Mass Spectrometry 37:9.
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Chinaza Godswill Awuchi, Maduabuchi Patrick Aja, Nancy Bonareri Mitaki, Sonia Morya, Ikechukwu O. Amagwula, Chinelo Kate Echeta & Victory S. Igwe. (2023) New Psychoactive Substances: Major Groups, Laboratory Testing Challenges, Public Health Concerns, and Community-Based Solutions. Journal of Chemistry 2023, pages 1-36.
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Nam Sook Kim, Hwan Seong Choi, Na Young Lim, Ji Hyun Lee, Hyungil Kim & Sun Young Baek. (2022) Application of Simultaneous Analytical Methods for Selective Androgen Receptor Modulator Adulterated in Dietary Supplements Advertised as Muscle Strengthening Using UHPLC-PDA and LC–ESI–MS/MS. Chromatographia 85:10-11, pages 895-919.
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Youquan Xie, Yucheng Tian, Yuming Zhang, Zhisheng Zhang, Rui Chen, Mian Li, Jiawei Tang, Jinlei Bian, Zhiyu Li & Xi Xu. (2022) Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998–2021). European Journal of Medicinal Chemistry 230, pages 114119.
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Pascal Kintz, Laurie Gheddar, Alice Ameline & Jean-Sébastien Raul. (2022) Human hair testing for selective androgen receptor modulators (SARMs): Current knowledge and limitations. Toxicologie Analytique et Clinique 34:1, pages 83-89.
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Pascal Kintz. (2022) The forensic response after an adverse analytical finding (doping) involving a selective androgen receptor modulator (SARM) in human athlete. Journal of Pharmaceutical and Biomedical Analysis 207, pages 114433.
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Pascal Kintz, Laurie Gheddar, Camille Paradis, Mickael Chinellato, Alice Ameline, Jean-Sébastien Raul & Magali Oliva-Labadie. (2021) Peroxisome Proliferator-Activated Receptor Delta Agonist (PPAR- δ) and Selective Androgen Receptor Modulator (SARM) Abuse: Clinical, Analytical and Biological Data in a Case Involving a Poisonous Combination of GW1516 (Cardarine) and MK2866 (Ostarine). Toxics 9:10, pages 251.
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Pascal KintzLaurie GheddarAlice AmelineJean-Sébastien Raul. (2021) Perspectives in Evaluating Selective Androgen Receptor Modulators in Human Hair: A Short Communication. Therapeutic Drug Monitoring 43:2, pages 298-300.
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Yat‐Ming So, Jenny K. Y. Wong, Timmy L. S. Choi, Anil Prabhu, Brian Stewart, Adrian F. Farrington, Paul Robinson, Terence S. M. Wan & Emmie N. M. Ho. (2020) Metabolic studies of selective androgen receptor modulators RAD140 and S‐23 in horses. Drug Testing and Analysis 13:2, pages 318-337.
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Pascal Kintz, Laurie Gheddar, Alice Ameline & Jean‐Sébastien Raul. (2020) Identification of S22 (ostarine) in human nails and hair using LC‐HRMS. Application to two authentic cases. Drug Testing and Analysis 12:10, pages 1508-1513.
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Emiliano Ventura, Anna Gadaj, Tom Buckley & Mark H. Mooney. (2020) Development of a multi‐residue high‐throughput UHPLC–MS/MS method for routine monitoring of SARM compounds in equine and bovine blood. Drug Testing and Analysis 12:9, pages 1373-1379.
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A. Z. Temerdashev & E. V. Dmitrieva. (2020) Methods for the Determination of Selective Androgen Receptor Modulators. Journal of Analytical Chemistry 75:7, pages 835-850.
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Anna Gadaj, Emiliano Ventura, Alexis Ripoche & Mark H. Mooney. (2019) Monitoring of selective androgen receptor modulators in bovine muscle tissue by ultra-high performance liquid chromatography-tandem mass spectrometry. Food Chemistry: X 4, pages 100056.
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Pascal Kintz, Alice Ameline, Laurie Gheddar & Jean-Sébastien Raul. (2019) LGD-4033, S-4 and MK-2866 – Testing for SARMs in hair: About 2 doping cases. Toxicologie Analytique et Clinique 31:1, pages 56-63.
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Christian M. Girgis. 2019. Osteosarcopenia: Bone, Muscle and Fat Interactions. Osteosarcopenia: Bone, Muscle and Fat Interactions 173 190 .
Argyro G. Fragkaki, Panagiotis Sakellariou, Polyxeni Kiousi, Nassia Kioukia‐Fougia, Maria Tsivou, Michael Petrou & Yiannis Angelis. (2018) Human in vivo metabolism study of LGD‐4033. Drug Testing and Analysis 10:11-12, pages 1635-1645.
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Robert Carrasquillo, Kevin Chu & Ranjith Ramasamy. (2018) Novel Therapy for Male Hypogonadism. Current Urology Reports 19:8.
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Mario Thevis & Wilhelm Schänzer. (2018) Detection of SARMs in doping control analysis. Molecular and Cellular Endocrinology 464, pages 34-45.
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Mario Thevis & Dietrich A Volmer. (2017) Mass spectrometric studies on selective androgen receptor modulators (SARMs) using electron ionization and electrospray ionization/collision-induced dissociation. European Journal of Mass Spectrometry 24:1, pages 145-156.
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Bianca Wiedemann, Jörn Weisner & Daniel Rauh. (2018) Chemical modulation of transcription factors. MedChemComm 9:8, pages 1249-1272.
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Mario Thevis, Thomas Piper, Josef Dib, Andreas Lagojda, Dirk Kühne, Lars Packschies, Hans Geyer & Wilhelm Schänzer. (2017) Mass spectrometric characterization of the selective androgen receptor modulator (SARM) YK-11 for doping control purposes. Rapid Communications in Mass Spectrometry 31:14, pages 1175-1183.
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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. (2017) 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. Bioorganic & Medicinal Chemistry 25:13, pages 3330-3349.
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Moriteru Asano, Takenori Hitaka, Takashi Imada, Masami Yamada, Megumi Morimoto, Hiromi Shinohara, Takahito Hara, Masuo Yamaoka, Takashi Santou, Masaharu Nakayama, Yumi Imai, Noriyuki Habuka, Jason Yano, Keith Wilson, Hisashi Fujita & Atsushi Hasuoka. (2017) Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part II: Optimization of 4-(pyrrolidin-1-yl)benzonitrile derivatives. Bioorganic & Medicinal Chemistry Letters 27:9, pages 1897-1901.
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Arthi Thirumalai, Kathryn E. Berkseth & John K. Amory. (2017) Treatment of Hypogonadism: Current and Future Therapies. F1000Research 6, pages 68.
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Christopher Wu & Jason R. Kovac. (2016) Novel Uses for the Anabolic Androgenic Steroids Nandrolone and Oxandrolone in the Management of Male Health. Current Urology Reports 17:10.
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Andreas Lagojda, Dirk Kuehne, Oliver Krug, Andreas Thomas, Tina Wigger, Uwe Karst, Wilhelm Schänzer & Mario Thevis. (2016) Identification of Selected in vitro -Generated Phase-I Metabolites of the Steroidal Selective Androgen Receptor Modulator MK-0773 for Doping Control Purposes . European Journal of Mass Spectrometry 22:2, pages 49-59.
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Bríd M. Ryan & Jessica M. Faupel-Badger. (2016) The hallmarks of premalignant conditions: a molecular basis for cancer prevention. Seminars in Oncology 43:1, pages 22-35.
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Mario Thevis, Andreas Lagojda, Dirk Kuehne, Andreas Thomas, Josef Dib, Annelie Hansson, Mikael Hedeland, Ulf Bondesson, Tina Wigger, Uwe Karst & Wilhelm Schänzer. (2015) Characterization of a non-approved selective androgen receptor modulator drug candidate sold via the Internet and identification of in vitro generated phase-I metabolites for human sports drug testing . Rapid Communications in Mass Spectrometry 29:11, pages 991-999.
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Kevin P. Cusack, Ying Wang, Michael Z. Hoemann, Jasmina Marjanovic, Roland G. Heym & Anil Vasudevan. (2015) Design strategies to address kinetics of drug binding and residence time. Bioorganic & Medicinal Chemistry Letters 25:10, pages 2019-2027.
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Christian M. Girgis. (2015) Integrated Therapies for Osteoporosis and Sarcopenia: From Signaling Pathways to Clinical Trials. Calcified Tissue International 96:3, pages 243-255.
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James G. MacKrell, Benjamin C. Yaden, Heather Bullock, Keyue Chen, Pamela Shetler, Henry U. Bryant & Venkatesh Krishnan. (2018) Molecular Targets of Androgen Signaling that Characterize Skeletal Muscle Recovery and Regeneration. Nuclear Receptor Signaling 13:1, pages nrs.13005.
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Mario Thevis & Wilhelm Schänzer. (2014) Analytical approaches for the detection of emerging therapeutics and non-approved drugs in human doping controls. Journal of Pharmaceutical and Biomedical Analysis 101, pages 66-83.
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Thomas Ullrich, Sanjita Sasmal, Venkatesham Boorgu, Srinivasu Pasagadi, Srisailam Cheera, Sujatha Rajagopalan, Archana Bhumireddy, Dhanya Shashikumar, Shekar Chelur, Charamanna Belliappa, Chetan Pandit, Narasimharao Krishnamurthy, Subhendu Mukherjee, Anuradha Ramanathan, Chakshusmathi Ghadiyaram, Murali Ramachandra, Paulo G. Santos, Bharat Lagu, Mark G. Bock, Mark H. Perrone, Sven Weiler & Hansjoerg Keller. (2014) 3-Alkoxy-pyrrolo[1,2- b ]pyrazolines as Selective Androgen Receptor Modulators with Ideal Physicochemical Properties for Transdermal Administration . Journal of Medicinal Chemistry 57:17, pages 7396-7411.
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Christian M. Girgis, Nancy Mokbel & Douglas J. DiGirolamo. (2014) Therapies for Musculoskeletal Disease: Can we Treat Two Birds with One Stone?. Current Osteoporosis Reports 12:2, pages 142-153.
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Xiaoping Yang & Aiying Guan. (2014) Application of fluorine-containing non-steroidal anti-androgen compounds in treating prostate cancer. Journal of Fluorine Chemistry 161, pages 1-10.
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Naoya Nagata, Kazuyuki Furuya, Nao Oguro, Daisuke Nishiyama, Kentaro Kawai, Noriko Yamamoto, Yuki Ohyabu, Masahiro Satsukawa & Motonori Miyakawa. (2013) Lead Evaluation of Tetrahydroquinolines as Nonsteroidal Selective Androgen Receptor Modulators for the Treatment of Osteoporosis. ChemMedChem 9:1, pages 197-206.
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