SERBA-2

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SERBA-2
SERBA-2.svg
Clinical data
Synonyms (2S,3R,4S)-SERBA[1]
Identifiers
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
Formula C18H18O3
Molar mass 282.34 g·mol−1
3D model (JSmol)

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[edit]

References[edit]

  1. ^ a b c 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. 
  2. ^ a b c 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. ^ a b c 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. 
  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. PMID 20738246. 
  5. ^ https://adisinsight.springer.com/drugs/800031986[permanent dead link]