Chemical compound
ERB-79 is a synthetic estrogen and a selective agonist of the ERβ .[ 1] [ 2] [ 3] It is a racemic mixture , with the active enantiomer being ERB-26 .[ 2] ERB-79 shows more than 484-fold selectivity for transactivation of the ERβ over the ERα.[ 1] Its EC50 value for the ERβ is 0.448 nM (14.52% of the potency of estradiol ) and for the ERα is 79 nM (0.03% of the potency of estradiol ).[ 1] It has no antagonistic activity at either receptor.[ 1] ERB-79 is active in preclinical models of arthritis .[ 1] The chemical structure of ERB-79 does not appear to have been disclosed.
^ a b c d e Dulos J, Vijn P, van Doorn C, Hofstra CL, Veening-Griffioen D, de Graaf J, Dijcks FA, Boots AM (2010). "Suppression of the inflammatory response in experimental arthritis is mediated via estrogen receptor α but not estrogen receptor β" . Arthritis Res. Ther . 12 (3): R101. doi :10.1186/ar3032 . PMC 2911889 . PMID 20497523 .
^ a b Attia DM, Ederveen AG (2012). "Opposing roles of ERα and ERβ in the genesis and progression of adenocarcinoma in the rat ventral prostate". Prostate . 72 (9): 1013–22. doi :10.1002/pros.21507 . PMID 22025007 . S2CID 12951793 .
^ Roa J, Vigo E, Castellano JM, Gaytan F, Navarro VM, Aguilar E, Dijcks FA, Ederveen AG, Pinilla L, van Noort PI, Tena-Sempere M (2008). "Opposite roles of estrogen receptor (ER)-α and ERβ in the modulation of luteinizing hormone responses to kisspeptin in the female rat: implications for the generation of the preovulatory surge" . Endocrinology . 149 (4): 1627–37. doi :10.1210/en.2007-1540 . PMID 18174277 .