11β-Methoxy-17-ethynyl-1,3,5(10)-estratriene-3,17β-diol (Moxestrol), a Tag for Estrogen Receptor Binding Sites in Human Tissues

摘要: Abstract A particularly simple, sensitive, and inexpensive technique has been developed for the routine assay of estrogen receptor binding sites in human tissues (endometrium breast cancer specimens) with use a radiolabeled potent estrogen, moxestrol [11β-methoxy-17-ethynyl-1,3,5(10)-estratriene-3,17β-diol]. In these binds specifically to which it forms stable complex that, at 25°, dissociates twice as slowly dose estradiol/receptor complex. Unlike estradiol not bind high affinity plasma sex steroid-binding protein. correlation analysis on 215 specimens, was found site concentrations, determinations carried out were extremely well correlated those performed (in presence dihydrotestosterone order minimize interference from protein). For low overestimated spite dihydrotestosterone. Thus, labeled instead improves accuracy measurement specific tissue binding. Satisfactory conditions dextran-coated charcoal adsorption exchange have this paper; maximum number are measured after incubation 2 10 nm radioligand 3 5 hr 25°.