SERBA-2
ナビゲーションに移動
検索に移動
| ファイル:SERBA-2.svg | |
|---|---|
| Systematic (IUPAC) name | |
| (3aR,4S,9bS)-4-(4-Hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 533884-10-5 |
| ATC code | ? |
| PubChem | CID 9925763 |
| ChemSpider | 8101398 |
| ChEMBL | CHEMBL216355 |
| Synonyms | (2S,3R,4S)-SERBA[1] |
| Chemical data | |
| Formula | C18H18O3 |
| |
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 Paterni I, Bertini S, Granchi C, Macchia M, Minutolo F (2013). "Estrogen receptor ligands: a patent review update". Expert Opin Ther Pat. 23 (10): 1247–71. doi:10.1517/13543776.2013.805206. PMID 23713677. S2CID 6259593.
- ↑ 2.0 2.1 2.2 Norman BH, Dodge JA, Richardson TI, Borromeo PS, Lugar CW, Jones SA, Chen K, Wang Y, Durst GL, Barr RJ, Montrose-Rafizadeh C, Osborne HE, Amos RM, Guo S, Boodhoo A, Krishnan V (2006). "Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia". J. Med. Chem. 49 (21): 6155–7. doi:10.1021/jm060491j. PMID 17034120.
- ↑ 3.0 3.1 3.2 Minutolo F, Macchia M, Katzenellenbogen BS, Katzenellenbogen JA (2011). "Estrogen receptor β ligands: recent advances and biomedical applications". Med Res Rev. 31 (3): 364–442. doi:10.1002/med.20186. PMID 19967775. S2CID 3841877.
- ↑ Lóránd T, Vigh E, Garai J (2010). "Hormonal action of plant derived and anthropogenic non-steroidal estrogenic compounds: phytoestrogens and xenoestrogens". Curr. Med. Chem. 17 (30): 3542–74. doi:10.2174/092986710792927813. PMID 20738246.
- ↑ "Erteberel - AdisInsight". adisinsight.springer.com. Archived from the original on 31 December 2016. Retrieved 15 January 2022.