Oestrogenic and antioestrogenic actions in a series of triphenylbut-1-enes: modulation of prolactin synthesis in vitro

British Journal of Pharmacology
V C JordanM R Schneider


The oestrogenic and antioestrogenic activities of a series of substituted derivatives of 1,1,2 triphenylbut-1-ene have been determined using primary cultures of rat pituitary gland cells to monitor prolactin synthesis in vitro. The relative binding affinity of the agonists for the oestrogen receptor was consistent with their oestrogenic potency. Bis para substitution at C1 of 1,1,2 triphenylbut-1-ene with either phenolic or acetoxy groups produced partial agonists. The antioestrogenic properties were reversible by the incubation of cells with increasing concentrations of oestradiol. The results lend support to a hypothetical single binding site model of oestrogen action, based upon an adaptation of Belleau's macromolecular perturbation theory.


Dec 1, 1978·Proceedings of the National Academy of Sciences of the United States of America·M E LiebermanJ Gorski
Jan 1, 1979·Fertility and Sterility·L C Huppert
Nov 1, 1977·The Journal of Endocrinology·V C JordanG Prestwich
Sep 1, 1985·Environmental Health Perspectives·V C JordanM E Lieberman
Feb 1, 1967·Journal of Reproduction and Fertility·M J Harper, A L Walpole
Jan 1, 1984·Pharmacology & Therapeutics·B J Furr, V C Jordan
Mar 1, 1982·Molecular and Cellular Endocrinology·M E LiebermanJ Gorski
Oct 1, 1960·Proceedings of the Society for Experimental Biology and Medicine·D E HOLTKAMPL J LERNER
Jul 1, 1947·The Journal of Endocrinology·C W EMMENS

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