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Binding of 17-alpha-ethinyl estradiol and mestranol to uterine and pituitary gland receptors of the rat in vitro
Authors:K Schubert  J Schlegel
Abstract:Comparative study, through radiochemical analysis, of the binding of estrogens to the uterine and pituitary receptors in immature rats showed that, for binding to the uterine recpetors, a free OH group in Position 3 is necessary. 17alpha-ethinyl estradiol as well as mestranol (17alpha-ethinyl estradiol-3-methyl ether), showed a stronger affinity for the pituitary than the uterine receptors. Indeed, mestranol, among the 3-methyl ether estrogens, has a special place in respect to its affinity for the pituitary. Since the binding to the receptors is an essential stage in inhibition or stimulation effects, this is a significant point. It may be that mestranol exercises its recognized central effect not only indirectly through release of ethinyl estradiol, but also directly.
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