The binding of radioactive estradiol to specific receptor protein in soluble fractions of uterine homogenates from rabbits is concentration dependent and is inhibited by the anti-estrogenic compounds, clomiphene and CL-868. The inhibition of estradiol binding is proportional to the concentration of these anti-estrogens. Clomiphene inhibits the binding of radioactive estradiol by slices of human myometrium and of rabbit uteri and prevents the transfer of the steroid from the receptors in the soluble fractions into the nuclear-myofibrillar extracts. Such systems may provide a means for the in vitro testing of some biochemical properties of anti-estrogenic compounds.
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WYSS et al. (1968) studied this question.