Benzopyrans are selective estrogen receptor Beta agonists with novel activity in models of benign prostatic hyperplasia.

Benzopyran selective estrogen receptor beta agonist-1 (SERBA-1) shows potent, selective binding and agonist function in estrogen receptor β (ERβ) in vitro assays. X-ray crystal structures of SERBA-1 in ERα and β help explain observed β-selectivity of this ligand. SERBA-1 in vivo demonstrates involution of the ventral prostate in CD-1 mice (ERβ effect), while having no effect on gonadal hormone levels (ERα effect) at 10× the efficacious dose, consistent with in vitro properties of this molecule.