Benzopyran selective estrogen receptor beta agonist-1(SERBA-1) shows potent, selective binding and agonist function inestrogen receptor
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(ER
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) in vitro assays. X-ray crystal structures ofSERBA-1 in ER
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and
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help explain observed
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-selectivity of thisligand. SERBA-1 in vivo demonstrates involution of the ventral prostatein CD-1 mice (ER
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effect), while having no effect on gonadal hormonelevels (ER
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effect) at 10× the efficacious dose, consistent with in vitroproperties of this molecule.