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Literature DB >> 24900290

Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140.

Chris P Miller¹, Maysoun Shomali¹, C Richard Lyttle¹, Louis St L O'Dea¹, Hillary Herendeen¹, Kyla Gallacher¹, Dottie Paquin¹, Dennis R Compton², Bishwabhusan Sahoo², Sean A Kerrigan², Matthew S Burge², Michael Nickels², Jennifer L Green², John A Katzenellenbogen³, Alexei Tchesnokov⁴, Gary Hattersley¹.

Abstract

This report describes the discovery of RAD140, a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). The characterization of RAD140 in several preclinical models of anabolic androgen action is also described.

Entities: Gene

Keywords: Androgen; Herschberger assay; SARM; cachexia; oxadiazole; primate

Year: 2010 PMID： 24900290 PMCID： PMC4018048 DOI： 10.1021/ml1002508

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

14 in total

1. Myotrophic activity of 19-nortestosterone and other steroids determined by modified levator ani muscle method.

Authors: L G HERSHBERGER; E G SHIPLEY; R K MEYER
Journal: Proc Soc Exp Biol Med Date: 1953-05

Review 2. Chemistry and structural biology of androgen receptor.

Authors: Wenqing Gao; Casey E Bohl; James T Dalton
Journal: Chem Rev Date: 2005-09 Impact factor: 60.622

Review 3. International Union of Pharmacology. LXV. The pharmacology and classification of the nuclear receptor superfamily: glucocorticoid, mineralocorticoid, progesterone, and androgen receptors.

Authors: Nick Z Lu; Suzanne E Wardell; Kerry L Burnstein; Donald Defranco; Peter J Fuller; Vincent Giguere; Richard B Hochberg; Lorraine McKay; Jack-Michel Renoir; Nancy L Weigel; Elizabeth M Wilson; Donald P McDonnell; John A Cidlowski
Journal: Pharmacol Rev Date: 2006-12 Impact factor: 25.468

Review 4. Ockham's razor and selective androgen receptor modulators (SARMs): are we overlooking the role of 5alpha-reductase?

Authors: Wenqing Gao; James T Dalton
Journal: Mol Interv Date: 2007-02

5. Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators.

Authors: Nathalie Schlienger; Birgitte W Lund; Jan Pawlas; Fabrizio Badalassi; Fabio Bertozzi; Rasmus Lewinsky; Alma Fejzic; Mikkel B Thygesen; Ali Tabatabaei; Stefania Risso Bradley; Luis R Gardell; Fabrice Piu; Roger Olsson
Journal: J Med Chem Date: 2009-11-26 Impact factor: 7.446

6. Body weight, alcohol consumption and liver enzyme activity--a 4-year follow-up study.

Authors: D H Lee; M H Ha; D C Christiani
Journal: Int J Epidemiol Date: 2001-08 Impact factor: 7.196

7. Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats.

Authors: Jacek Ostrowski; Joyce E Kuhns; John A Lupisella; Mark C Manfredi; Blake C Beehler; Stanley R Krystek; Yingzhi Bi; Chongqing Sun; Ramakrishna Seethala; Rajasree Golla; Paul G Sleph; Aberra Fura; Yongmi An; Kevin F Kish; John S Sack; Kasim A Mookhtiar; Gary J Grover; Lawrence G Hamann
Journal: Endocrinology Date: 2006-09-28 Impact factor: 4.736

8. Assessment of fertility in male rats after extended chemical castration with a GnRH antagonist.

Authors: Susan S D'Souza; Francesca Selmin; Santos B Murty; Wei Qiu; B C Thanoo; Patrick P DeLuca
Journal: AAPS PharmSci Date: 2004-03-11

9. 1,3,4-Oxadiazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 2: SAR of the C5 position.

Authors: Brian A Johns; Jason G Weatherhead; Scott H Allen; James B Thompson; Edward P Garvey; Scott A Foster; Jerry L Jeffrey; Wayne H Miller
Journal: Bioorg Med Chem Lett Date: 2009-01-30 Impact factor: 2.823

10. Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications.

Authors: James J Li; James C Sutton; Alexandra Nirschl; Yan Zou; Haixia Wang; Chongqing Sun; Zulan Pi; Rebecca Johnson; Stanley R Krystek; Ramakrishna Seethala; Rajasree Golla; Paul G Sleph; Blake C Beehler; Gary J Grover; Aberra Fura; Viral P Vyas; Cindy Y Li; Jack Z Gougoutas; Michael A Galella; Robert Zahler; Jacek Ostrowski; Lawrence G Hamann
Journal: J Med Chem Date: 2007-06-07 Impact factor: 7.446

9 in total

Review 1. Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications.

Authors: Zachary J Solomon; Jorge Rivera Mirabal; Daniel J Mazur; Taylor P Kohn; Larry I Lipshultz; Alexander W Pastuszak
Journal: Sex Med Rev Date: 2018-11-30

2. SAR Studies on Aromatic Acylhydrazone-Based Inhibitors of Fungal Sphingolipid Synthesis as Next-Generation Antifungal Agents.

Authors: Krupanandan Haranahalli; Cristina Lazzarini; Yi Sun; Julia Zambito; Senuri Pathiranage; J Brian McCarthy; John Mallamo; Maurizio Del Poeta; Iwao Ojima
Journal: J Med Chem Date: 2019-08-16 Impact factor: 7.446

3. Could Overt Diabetes Be Triggered by Abuse of Selective Androgen Receptor Modulators and Growth Hormone Secretagogues? A Case Report and Review of the Literature.

Authors: Richard Sotorník; Roguel Suissa; Jean-Luc Ardilouze
Journal: Clin Diabetes Date: 2022

9. Human In Vivo Metabolism and Elimination Behavior of Micro-Dosed Selective Androgen Receptor Modulator RAD140 for Doping Control Purposes.

Authors: Felicitas Wagener; Luisa Euler; Christian Görgens; Sven Guddat; Mario Thevis
Journal: Metabolites Date: 2022-07-20