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LGD 3303 is a selective androgen receptor modulator (SARM; Ki = 0.9 nM).1 It selectively binds to the androgen receptor over the mineralocorticoid, glucocorticoid, and progesterone receptors (Kis = 1,261, 581, and 136 nM, respectively). LGD 3303 also selectively activates the androgen receptor over the mineralocorticoid and progesterone receptors in reporter assays using CV-1 cells (EC50s = 3.6, 3,695, and 2,233 nM, respectively). It increases levator ani muscle mass, but not prostate muscle mass, in orchiectomized (ORDX) rats at 3 mg/kg per day. LGD 3303 increases body weight and gastrocnemius mass, bone mineral content and density in the lumbar spine and mid-femur, and bone formation rate in ovariectomized (OVX) rats. It increases time spent near male rats by sexually experienced, hormone-primed OVX female rats but decreases time spent near male rats by sexually naïve, hormone-primed OVX female rats, in sexual preference tests.2
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1. Combination treatment with a selective androgen receptor modulator (SARM) and a bisphosphonate has additive effects in osteopenic female rats. J. Bone Miner. Res. 24(2), 231-240 (2009).
2. A selective androgen receptor modulator enhances male-