Novel plasma membrane action of estrogen and antiestrogens revealed by their regulation of a large conductance chloride channel

Antiestrogens antagonize many genomic effects of estrogen through binding to the nuclear estrogen receptor. We report here that NIH3T3 fibroblasts grown in the presence of colchicine acquire the activation of a large conductance chloride channel upon exposure to extracellular but not intracellular antiestrogens. This effect can be prevented by extracellular 17β‐estradiol, but not intracellular 17β‐estradiol or extracellular 17α‐estradiol. This is the first demonstration of a regulatory role for antiestrogens and estrogens in the regulation of ionic channels occurring through an interaction of these compounds with a plasma membrane binding site distinct from the classical estrogen receptor and subsequent activation of intracellular second messenger pathway (or pathways).— Hardy, S. P., Valverde, M. A. Novel plasma membrane action of estrogen and antiestrogens revealed by their regulation of a large conductance chloride channel. FASEB J. 8: 760‐765; 1994.

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