Methyltrienolone, a specific ligand for cellular androgen receptors.
Methyltrienolone (R 1881), 17beta-hydroxy-17alpha-methyl-estra-4,9,11-trien-3-one, a very active androgen, binds specifically to rat prostate cytosol with a higher affinity than androstanolone. Unlike the physiological hormone, however, it is not bound by human sex steroid plasma binding protein, SBP. This specific ligand is thus a useful tool for the detection of elusive androgen receptors and for their study, for instance, in human tumors where interference from plasma contamination has to be circumvented.
D000818:Animals; D001667:Binding, Competitive; D001798:Blood Proteins / Q000378:metabolism; D003600:Cytosol / Q000378:metabolism; D013196:Dihydrotestosterone / Q000378:metabolism; D004963:Estrenes / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D008297:Male; D011467:Prostate / Q000378:metabolism; D011485:Protein Binding; D051381:Rats; D011956:Receptors, Cell Surface; D045165:Testosterone Congeners / Q000378:metabolism*
D001798:Blood Proteins; D004963:Estrenes; D011956:Receptors, Cell Surface; D045165:Testosterone Congeners; D013196:Dihydrotestosterone