WAY-214156 is a synthetic nonsteroidal estrogen that acts as a highly selective agonist of the ERβ.[1][2] It is 100-fold selective for the ERβ over the ERα with an IC50 of 4.2 nM (compare to estradiol with IC50 values of ~3–4 nM for both the ERα and ERβ).[1] The drug is less selective for the ERβ than is prinaberel (ERB-041, WAY-202041), another selective ERβ agonist, but is more potent in comparison.[1] WAY-214156 may produce anti-inflammatory effects via the ERβ and has been proposed as a potential treatment for inflammatory conditions such as rheumatoid arthritis.[1][3]
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| Formula | C19H10N2O3 |
| Molar mass | 314.300 g·mol−1 |
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See also
editReferences
edit- ^ a b c d Cvoro A, Tatomer D, Tee MK, Zogovic T, Harris HA, Leitman DC (January 2008). "Selective estrogen receptor-beta agonists repress transcription of proinflammatory genes". Journal of Immunology. 180 (1): 630–636. doi:10.4049/jimmunol.180.1.630. PMID 18097065.
- ^ Serock MR, Wells AK, Khalil RA (November 2008). "Modulators of vascular sex hormone receptors and their effects in estrogen-deficiency states associated with menopause". Recent Patents on Cardiovascular Drug Discovery. 3 (3): 165–186. doi:10.2174/157489008786263970. PMID 18991792.
- ^ Roman-Blas JA, Castañeda S, Cutolo M, Herrero-Beaumont G (November 2010). "Efficacy and safety of a selective estrogen receptor β agonist, ERB-041, in patients with rheumatoid arthritis: a 12-week, randomized, placebo-controlled, phase II study". Arthritis Care & Research. 62 (11): 1588–1593. doi:10.1002/acr.20275. PMID 20556817. S2CID 19511497.
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