Estrogen receptor translocation and replenishment in rat hypothalamus and pituitary gland after the application of catecholestrogen or nonsteroidal antiestrogen

Abstract The time course of nuclear translocation of estrogen receptors and the replenishment of cytosolic receptor concentrations in the pituitary gland and hypothalamus of ovariectomized/adrenalectomized rats after the application of a high dose (0.1 mg/animal) of the catecholestrogens, 2-hydroxyethynylestradiol or 4-hydroxyethynylestradiol, was identical to that seen after the application of the monophenolic estrogen 17α-ethynylestradiol. A distinctly different pattern of receptor distribution between these cell compartments was observed after the application of the nonsteroidal antiestrogen monohydroxytamoxifen (ICI 79,280) resulting in a prolonged depletion of cytosolic receptor concentrations. It therefore seems unlikely that the proposed antiestrogenic properties of 2-hydroxyestrogens are the result of a blocking of cytosolic receptor replenishment but may be explained by a reduced intrinsic nuclear activity of estrogen receptors complexed with 2-hydroxyestrogens.