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.
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| Drug class | Estrogen; Selective ERβ agonist |
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See also
editReferences
edit- ^ 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.
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