A diphenylmethane derivative specific for the antiestrogen binding site found in rat liver microsomes.
A new para-diphenylmethyl derivative, N,N-diethyl-2-[(4-phenylmethyl)-phenoxy]-ethanamine X HCl (N,N-DPPE) has been synthesized which binds with high affinity to the anti-estrogen binding site found in male rat liver microsomes. However, no evidence of significant interaction with the estrogen receptor can be observed at or below 10 microM in rat uterine cytosols; 10 nM N,N-DPPE fails to significantly induce progesterone receptor in MCF-7 cells. Tamoxifen also binds to anti-estrogen binding site but, unlike N,N-DPPE, binds significantly to estrogen receptor at much lower concentrations and induces MCF-7 progesterone receptor. This property of high affinity for anti-estrogen binding site but not for estrogen receptor may make N,N-DPPE an important probe for the study of anti-estrogen binding site and its biological relevance.
D000818:Animals; D001667:Binding, Competitive; D001943:Breast Neoplasms / Q000378:metabolism; D004958:Estradiol / Q000378:metabolism; D005260:Female; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism*; D010647:Phenyl Ethers / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011955:Receptors, Drug; D011960:Receptors, Estrogen / Q000378:metabolism*; D011980:Receptors, Progesterone / Q000378:metabolism; D013629:Tamoxifen / Q000378:metabolism
D010647:Phenyl Ethers; D011955:Receptors, Drug; D011960:Receptors, Estrogen; D011980:Receptors, Progesterone; D013629:Tamoxifen; D004958:Estradiol; C043062:tesmilifene