Pharmacodynamics of Selective Androgen Receptor Modulators
- D. Yin, Wenqing Gao, J. Dalton
- Biology, MedicineJournal of Pharmacology and Experimental…
- 1 March 2003
Compounds S-1 and S-4 were identified as SARMs with potent and tissue-selective in vivo pharmacological activity, and represent the first members of a new class of SAR Ms with selective anabolic effects.
Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5alpha-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: new…
- Wenqing Gao, J. D. Kearbey, J. Dalton
- Biology, MedicineEndocrinology
- 1 December 2004
Although S-1 and finasteride showed very similar suppressive effects in the prostate of intact male rats, they decreased prostate size via different mechanisms of action, indicating that SARMs may demonstrate clinical utility as single agent or combination therapy for BPH.
Selective androgen receptor modulator treatment improves muscle strength and body composition and prevents bone loss in orchidectomized rats.
- Wenqing Gao, P. Reiser, J. Dalton
- Biology, MedicineEndocrinology
- 1 November 2005
The strong anabolic effects of S-4 in skeletal muscle, bone, and pituitary were achieved with minimal pharmacologic effect in the prostate and demonstrates the promising therapeutic utility that this new class of drugs may hold.
Structural Determinants of P-Glycoprotein-Mediated Transport of Glucocorticoids
- C. R. Yates, Cheng Chang, P. Swaan
- Biology, ChemistryPharmaceutical Research
- 1 November 2003
Three-dimensional structure-activity relationships were built to determine how specific structural features within the steroids affect their P-gp-mediated efflux, demonstrating the importance of glucocorticoid structure to P-glycoprotein transport.
Selective Androgen Receptor Modulator (SARM) Treatment Prevents Bone Loss and Reduces Body Fat in Ovariectomized Rats
- J. D. Kearbey, Wenqing Gao, J. Dalton
- BiologyPharmaceutical Research
- 1 February 2007
The data suggest that S-4 could reduce the incidence of fracture via two different mechanisms (i.e., via direct effects in bone and reducing the occurrence of falls through increased muscle strength).
Estrogen Receptor-β-selective Ligands Alleviate High-fat Diet- and Ovariectomy-induced Obesity in Mice
- Muralimohan Yepuru, J. Eswaraka, R. Narayanan
- Biology, MedicineJournal of Biological Chemistry
- 23 July 2010
Assessment of the pharmacological effect of ER-β-selective ligands in animal models of high-fat diet- and ovariectomy-induced obesity indicates that ligand-activated ER- β is a potential therapeutic target to combat obesity and obesity-related metabolic diseases.
Steroidal androgens and nonsteroidal, tissue-selective androgen receptor modulator, S-22, regulate androgen receptor function through distinct genomic and nongenomic signaling pathways.
- R. Narayanan, C. Coss, Muralimohan Yepuru, J. D. Kearbey, Duane D. Miller, J. Dalton
- Biology, ChemistryMolecular Endocrinology
- 1 November 2008
Comparisons and in vitro studies reveal novel differences in the molecular mechanisms by which S-22, a nonsteroidal SARM, and DHT mediate their pharmacological effects.
MicroRNAs Are Mediators of Androgen Action in Prostate and Muscle
- R. Narayanan, Jinmai Jiang, J. Dalton
- Biology, MedicinePLoS ONE
- 27 October 2010
A feedback loop between miRs, corepressors and AR and the imperative role of miRs in AR function in non-cancerous androgen-responsive tissues are demonstrated.
Characterization of in vitro generated metabolites of the selective androgen receptor modulators S-22 and S-23 and in vivo comparison to post-administration canine urine specimens.
- M. Thevis, E. Gerace, W. Schänzer
- Biology, ChemistryDrug Testing and Analysis
- 1 November 2010
The structure of analytically useful urinary metabolites should be elucidated to provide targets for sensitive and retrospective analysis and M3 was chemically synthesized, characterized by nuclear magnetic resonance spectroscopy and high resolution/high accuracy mass spectrometry, and chosen as primary target for future doping control analyses.
Pharmacokinetics of S-3-(4-acetylamino-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro- 3-trifluoromethyl-phenyl)-propionamide in rats, a non-steroidal selective androgen receptor modulator
- J. D. Kearbey, D. Wu, Wei Gao, D. Miller, J. Dalton
- Biology, MedicineXenobiotica; the fate of foreign compounds in…
- 1 March 2004
The pharmacokinetics and oral bioavailability of S-4 indicate that it is an excellent candidate for clinical development and rapidly absorbed, slowly cleared, and has a moderate volume of distribution in rats.
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