Selective Androgen Receptor Modulators SARMs

SARMs Nucleus Representative Compound MolWt (Da) Precursor Ion (m/z) Product Ions m/z)  

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Structural modifications of bicalutamide led to the discovery of the first generation of selective androgen receptor modulators (SARMs). These compounds not only bind to the AR with an affinity in the nanomolar range, but they also show tissue selectivity in animal models [206]. 

Brown TR. Nonsteroidal selective androgen receptors modulators (SARMs) designer androgens with flexible structures provide clinical promise. Endocrinology 2004 145 5417-5419. 

Rosen, J. and Negro-Vilar, A. (2002) Novel, non-steroidal, selective androgen receptor modulators (SARMs) with anabolic activity in bone and muscle and improved safety profile. Journal of Musculoskeletal and Neuronal Interactions, 32, 222-224. 

Arylisothiocyanato selective androgen receptor modulators (SARMs) for prostate cancer. Bioorganic and Medicinal Chemistry, 14, 6525-6538. 

Kearbey, J.D., Gao, W., Narayanan, R., Fisher, S.J., Wu, D., Miller, D.D. and Dalton, J.T. (2007) Selective androgen receptor modulator (SARM) treatment prevents bone loss and reduces body fat in ovariectomized rats. Pharmaceutical Research, 24, 328-335. 

T., Miyakawa, M., Amano, S., Sumita, Y. and Oguro, N. (2003) Bone anabolic effects of S-40503, a novel nonsteroidal selective androgen receptor modulator (SARM), in rat models of osteoporosis. Biological e[ Pharmaceutical Bulletin, 26, 1563-1569. 

Ke, H.Z., Crawford, D.T., Qi, H. et al. (23-27 September 2005) Differential effects of 5a-dihydrotestosterone (DHT) and a novel selective androgen receptor modulator (SARM) on prostate and bone in intact and orchidectomized (ORX) male rats, 27th Annual Meeting of the American Society for Bone and Mineral Research, abstract M395. 

Han, B., Triantafillou, J.A., Shen, Y., Xu, T., Scates, P., Stimpson, S.A. and Turnbull, P.S. (2-5 June 2007) Pharmacological profiles of GSK2420A, a novel nonsteroidal selective androgen receptor modulator (SARM), Endocrine... 

Ng, R.A., Lanter, J.C., Alford, V.C., Allan, G.F., Sbriscia, T., Lundeen, S.G. and Sui, Z. (2007) Synthesis of potent and tissue-selective androgen receptor modulators (SARMs) 2-(2,2,2)-trifluoroethyl-benzimidazole scaffold. Bioorganic el Medicinal Chemistry Letters, 17, 1784-1787. 

Figure 3.15 Structure of the selective androgen receptor modulator (SARM) (8).

Negro-Vilar, A. (1999) Selective androgen receptor modulators (SARMs) A novel approach to androgen therapy for the new millennium. Journal of Clinical Endocrinology and Metabolism, 84,3459-3462. 

SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMs) 173 TABLE 4.4 Characteristic Product Ions of Selected SARMs Generated by ESI and CID... 

Wu, D., Wu, Z., Yang, J., et al. (2006) Pharmacokinetics and metabolism of a selective androgen receptor modulator (SARM) in rats—Implication of molecular properties and intensive metabolic profile to investigate ideal pharmacokinetic characteristics of a propanamide in preclinical study. Drug Metabolism and Disposition, 34,483-494. 

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