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SERBA-2

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
SERBA-2
Clinical data
Other names(2S,3R,4S)-SERBA[1]
Identifiers
  • (3aR,4S,9bS)-4-(4-Hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol
CAS Number
PubChemCID
ChemSpider
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC18H18O3
Molar mass282.339 g·mol−1
3D model (JSmol)
  • C1C[C@@H]2[C@H](C1)C3=C(C=CC(=C3)O)O[C@@H]2C4=CC=C(C=C4)O
  • InChI=1S/C18H18O3/c19-12-6-4-11(5-7-12)18-15-3-1-2-14(15)16-10-13(20)8-9-17(16)21-18/h4-10,14-15,18-20H,1-3H2/t14-,15+,18+/m0/s1
  • Key:XIESSJVMWNJCGZ-HDMKZQKVSA-N

SERBA-2, short forselective estrogen receptor beta agonist-2, is asynthetic,nonsteroidalestrogen which acts as a selectiveERβagonist.[2][3] For theERα and ERβ, SERBA-2 hasaffinities (Ki) of 14.5 nM and 1.54 nM,efficacies of 85% and 100%, andEC50 values of 85 nM and 3.61 nM, respectively, demonstrating 9-foldbinding selectivity and 11-foldfunctional selectivity for the ERβ over the ERα.[2][3][4][1] Anenantiomer of SERBA-2,erteberel (SERBA-1), is morepotent and selective in comparison and is under development for the treatment ofschizophrenia.[5][2][3][1]

See also

[edit]

References

[edit]
  1. ^abcPaterni 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. ^abcNorman 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. ^abcMinutolo 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.
  4. ^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.
  5. ^"Erteberel - AdisInsight".adisinsight.springer.com. Archived fromthe original on 31 December 2016. Retrieved15 January 2022.
ERTooltip Estrogen receptor
Agonists
Mixed
(SERMsTooltip Selective estrogen receptor modulators)
Antagonists
GPERTooltip G protein-coupled estrogen receptor
Agonists
Antagonists
Unknown


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