ERB-79
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
References
- 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 alpha but not estrogen receptor beta". Arthritis Res. Ther. 12 (3): R101. doi:10.1186/ar3032. PMC 2911889. PMID 20497523.
- 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)-alpha and ERbeta 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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