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504421 
Journal Article 
Anti-osteopenic effect of benzo b furan derivative MU314: evaluation as novel SERM-like compound 
Nakamuta, H; Fukuyama, R; Fujita, M; Kodama, Y; Shimokawa, A; Sano, R; Koida, M; Ando, K; Ohishi, Y 
2005 
1 
Yakugaku Zasshi
ISSN: 0031-6903
EISSN: 1347-5231 
125 
102-103 
Japanese 
Raloxifene (Ral) is a selective estrogen receptor modulator (SERM) and recently marketed anti-osteoporotic drug that acts on estrogen receptors to exert a variety of estrogen-like actions in a tissue-specific manner, some therapeutic but other unwanted. A novel series of benzo[6]furan compounds (BF) were synthesized and first screened for the anti-bone resorption potency in vitro. MU-314(5-bromo-2-(4-chlorobenzoyl) -3-[(2)-(2-cyano-3-hydroxybut-2-enonyl)amino]benzo[Z)]furan, based on its p-estra-diol(E 2)-potency in 10 nM, was selected for in vivo assay using OVX rats. MU'314(100 jig/kg, s.c. 4 times/wk) suppressed OVX-induced reductions of BMD and mechanical strength of femoral head as E 2 did, but without reversing OVX-induced uterine atrophy. The results show that MU314 may lead us to a novel series of SERM-like anti-osteoporotics. 
SERM; osteoporosis; estrogen; bone resorption