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Chemical Compound Review:

NITROMIFENE 1-[2-[4-[(Z)-1-(4- methoxyphenyl)-2-nitro-2...

Synonyms: Nitromifeno, Nitromifenum, Nitromiphene, AC1MHUBN, CHEMBL2105203, ...

Ruenitz, P.C. et al., Hiemke, C. et al.

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Disease relevance of NITROMIFENE

Characterization of MCF 7 breast cancer cell growth inhibition by the antiestrogen nitromifene (CI 628) and selected metabolites [1].

High impact information on NITROMIFENE

Besides undergoing O-demethylation in vivo, the triarylethylene antiestrogen nitromifene [1-(4-(2-pyrrolidinylethoxy)phenyl)-1-(4-methoxy)-phenyl-2-phenyl- 2- nitroethene, 1] undergoes biotransformation via nitroreduction, ethene bond cleavage, and pyrrolidine ring oxidation affording ketone metabolites 2 and 3 and a lactam metabolite 4 [1].
The non-steroidal triphenylethylene-type antiestrogens with an amine side chain--enclomiphene, nitromifene, tamoxifen and zuclomiphene--were found to be competitive inhibitors of [3H]spiroperidol (Kd = 0.12 nM; Bmax = 101 fmol/mg protein) and [3H]domperidone (Kd = 0.62 nM; Bmax = 86 fmol/mg protein) binding to striatal membranes [2].

References

Characterization of MCF 7 breast cancer cell growth inhibition by the antiestrogen nitromifene (CI 628) and selected metabolites. Ruenitz, P.C., Thompson, C.B., Srivatsan, V. J. Steroid Biochem. (1989) [Pubmed]
Interaction of non-steroidal antiestrogens with dopamine receptor binding. Hiemke, C., Ghraf, R. J. Steroid Biochem. (1984) [Pubmed]

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