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ERB-79
Clinical data
Drug class Estrogen; Selective ERβ agonist
Identifiers
CAS Number

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.

See also

References

  1. ^ 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.
  2. ^ 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.
  3. ^ 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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