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

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Norman BH, Dodge JA, Richardson TI, Borromeo PS, Lugar CW, Jones SA, Chen K, Wang Y, Durst GL, Barr RJ, Montrose-Rafizadeh C, Osborne HE, Amos RM, Guo S, Boodhoo A, Krishnan V

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

J Med Chem. 2006 Oct 19;49(21):6155-7.

PubMed ID
17034120 [ View in PubMed
]
Abstract

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ErteberelEstrogen receptor alphaKi (nM)2.687.522Details
ErteberelEstrogen receptor alphaEC 50 (nM)19.47.522Details
ErteberelEstrogen receptor betaKi (nM)0.197.522Details
ErteberelEstrogen receptor betaEC 50 (nM)0.667.522Details