Nitromifene

From Wikipedia, the free encyclopedia
Jump to navigation Jump to search
Nitromifene
Nitromifene.svg
Clinical data
Other namesCI-628; CN-5518; CN-55945
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC27H28N2O4
Molar mass444.531 g·mol−1
3D model (JSmol)

Nitromifene (INN; also as the citrate salt nitromifene citrate (USAN), developmental code names CI-628, CN-5518, CN-55945) is a nonsteroidal selective estrogen receptor modulator (SERM) related to triphenylethylenes like tamoxifen that was never marketed.[1] It is a mixture of (E)- and (Z)-isomers that possess similar antiestrogenic activity.[2] The drug was described in 1966.[1] Along with tamoxifen, nafoxidine, and clomifene, it was one of the earliest SERMs.[3]

Nitromifene has been found to dissociate from the estrogen receptor 250-fold faster than estradiol.[4] This may be involved in its antagonistic activity at the estrogen receptor.[4]

References[edit]

  1. ^ a b J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 880–. ISBN 978-1-4757-2085-3.
  2. ^ Raymond Eller Kirk; Donald Frederick Othmer (1980). Encyclopedia of chemical technology. Wiley. p. 676. ISBN 978-0-471-02065-3.
  3. ^ Jordan VC, Morrow M (1999). "Tamoxifen, raloxifene, and the prevention of breast cancer". Endocr. Rev. 20 (3): 253–78. doi:10.1210/edrv.20.3.0368. PMID 10368771.
  4. ^ a b De Boer W, Notides AC, Katzenellenbogen BS, Hayes JR, Katzenellenbogen JA (January 1981). "The capacity of the antiestrogen CI-628 to activate the estrogen receptor in vitro". Endocrinology. 108 (1): 206–12. doi:10.1210/endo-108-1-206. PMID 7007019.