Chemistry:SERBA-2
From HandWiki
Short description: Chemical compound
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| Other names | (2S,3R,4S)-SERBA[1] |
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| Formula | C18H18O3 |
| Molar mass | 282.339 g·mol−1 |
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SERBA-2, short for selective estrogen receptor beta agonist-2, is a synthetic, nonsteroidal estrogen which acts as a selective ERβ agonist.[2][3] For the ERα and ERβ, SERBA-2 has affinities (Ki) of 14.5 nM and 1.54 nM, efficacies of 85% and 100%, and EC50 values of 85 nM and 3.61 nM, respectively, demonstrating 9-fold binding selectivity and 11-fold functional selectivity for the ERβ over the ERα.[2][3][4][1] An enantiomer of SERBA-2, erteberel (SERBA-1), is more potent and selective in comparison and is under development for the treatment of schizophrenia.[5][2][3][1]
See also
References
- ↑ 1.0 1.1 1.2 "Estrogen receptor ligands: a patent review update". Expert Opin Ther Pat 23 (10): 1247–71. 2013. doi:10.1517/13543776.2013.805206. PMID 23713677.
- ↑ 2.0 2.1 2.2 "Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia". J. Med. Chem. 49 (21): 6155–7. 2006. doi:10.1021/jm060491j. PMID 17034120.
- ↑ 3.0 3.1 3.2 "Estrogen receptor β ligands: recent advances and biomedical applications". Med Res Rev 31 (3): 364–442. 2011. doi:10.1002/med.20186. PMID 19967775.
- ↑ "Hormonal action of plant derived and anthropogenic non-steroidal estrogenic compounds: phytoestrogens and xenoestrogens". Curr. Med. Chem. 17 (30): 3542–74. 2010. doi:10.2174/092986710792927813. PMID 20738246.
- ↑ "Erteberel - AdisInsight". https://adisinsight.springer.com/drugs/800031986.
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