National Center for
2I0G: Benzopyrans Are Selective Estrogen Receptor Beta Agonists (serbas) With Novel Activity In Models Of Benign Prostatic Hyperplasia
Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia
J. Med. Chem. (2006) 49 p.6155-6157
Benzopyran selective estrogen receptor beta agonist-1 (SERBA-1) shows potent, selective binding and agonist function in estrogen receptor beta (ERbeta) in vitro assays. X-ray crystal structures of SERBA-1 in ERalpha and beta help explain observed beta-selectivity of this ligand. SERBA-1 in vivo demonstrates involution of the ventral prostate in CD-1 mice (ERbeta effect), while having no effect on gonadal hormone levels (ERalpha effect) at 10x the efficacious dose, consistent with in vitro properties of this molecule.