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