Cis isomer of centchroman--a selective ligand for the microsomal antiestrogen binding site.
Several compounds structurally related to the triarylethylene antiestrogens, but possessing weak estrogen receptor affinities, were assessed for their ability to interact with the microsomal antiestrogen binding site. While all the compounds tested did interact with this site their relative affinities were somewhat lower than that of tamoxifen. One of these, viz., the cis isomer of centchroman, has however emerged as a selective ligand for the antiestrogen binding site since its estrogen receptor affinity is nearly 50,000 times lower on a relative scale.
D000818:Animals; D001578:Benzopyrans / Q000378:metabolism*; D002486:Centchroman / Q000378:metabolism*; D005260:Female; D007536:Isomerism; D008861:Microsomes / Q000378:metabolism*; D008862:Microsomes, Liver / Q000378:metabolism; D051381:Rats; D011955:Receptors, Drug; D011960:Receptors, Estrogen / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014599:Uterus / Q000378:metabolism
D001578:Benzopyrans; D011955:Receptors, Drug; D011960:Receptors, Estrogen; D002486:Centchroman