LGD-3303 is an orally active, non-steroidal selective androgen receptor modulator (SARM) with high affinity for the androgen receptor (Ki=0.9nM)[1, 2]. LGD-3303 binds to the mineralocorticoid receptor, glucocorticoid receptor, and progesterone receptor with much lower affinity than to the androgen receptor (Ki=1261, 581, and 136nM, respectively)[3]. LGD-3303 was designed to selectively activate the androgen receptor (AR) signaling pathway in muscle and other tissues, aiming to maintain anabolic (muscle-building) effects while minimizing androgen-related side effects on tissues such as the prostate[4].
In vivo studies in Sprague-Dawley rats showed that oral administration of LGD-3303 (3 or 30mg/kg/day) for 7 days significantly enhanced sexual preference for males in female rats, but only in sexually experienced females[5].
References:
[1] Vajda E G, López F J, Rix P, et al. Pharmacokinetics and pharmacodynamics of LGD-3303, an orally available nonsteroidalselective androgen receptor modulator[J]. Journal of Pharmacology and Experimental Therapeutics, 2009, 328(2): 663.
[2] Zhang X, Sui Z. Deciphering the selective androgen receptor modulators paradigm[J]. Expert opinion on drug discovery, 2013, 8(2): 191-218.
[3] Vajda E G, Hogue A, Griffiths K N, et al. Combination treatment with a selective androgen receptor modulator q (SARM) and a bisphosphonate has additive effects in osteopenic female rats[J]. Journal of Bone and Mineral Research, 2009, 24(2): 231-240.
[4] Clarke B L, Khosla S. Modulators of androgen and estrogen receptor activity[J]. Critical Reviews™ in Eukaryotic Gene Expression, 2010, 20(4).
[5] Kudwa A E, López F J, McGivern R F, et al. A selective androgen receptor modulator enhances male-directed sexual preference, proceptive behavior, and lordosis behavior in sexually experienced, but not sexually naive, female rats[J]. Endocrinology, 2010, 151(6): 2659-2668.
LGD-3303是一种口服的非甾体选择性雄激素受体调节剂（SARM），与雄激素受体具有高亲和力（Ki=0.9nM）[1, 2]。LGD-3303与矿物质皮质醇受体、糖皮质醇受体和孕激素受体的结合亲和力远低于与雄激素受体的结合亲和力（分别为Ki=1261、581和136nM）[3]。LGD-3303被设计用于选择性激活肌肉和组织中的雄激素受体（AR）通路，以期在维持合成代谢（肌肉增长）效应的同时，尽可能减少对前列腺等组织的雄激素副作用[4]。
在体内，LGD-3303（3, 30mg/kg/day）通过口服处理SD大鼠7天，显著增强了雌性对雄性的性偏好，但仅限于有性经验的雌性[5]。