Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator.

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Piu F, Gardell LR, Son T, Schlienger N, Lund BW, Schiffer HH, Vanover KE, Davis RE, Olsson R, Bradley SR

Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator.

J Steroid Biochem Mol Biol. 2008 Mar;109(1-2):129-37. doi: 10.1016/j.jsbmb.2007.11.001. Epub 2007 Nov 22.

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18164613 [ View in PubMed
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Abstract

Because of the limitations and liabilities of current testosterone therapies, non-steroidal tissue-selective androgen receptor modulators may provide a clinically meaningful advance in therapy. Using a functional cell-based assay AC-262536 was identified as a potent and selective AR ligand, with partial agonist activity relative to the natural androgen testosterone. A 2-week chronic study in castrated male rats indicated that AC-262536 significantly improves anabolic parameters in these animals, especially in stimulating the growth of the levator ani and in suppressing elevated LH levels. In sharp contrast to testosterone, AC-262536 has weak androgenic effects, as measured by prostate and seminal vesicle weights. Thus, AC-262536 represents a novel class of selective androgen receptor modulators (SARMs) with beneficial anabolic effects.

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