The effect of analgin on glucocorticoid receptors

Golikov, P.P.; Nikolaeva, N.I.

Eksperimental'naia i Klinicheskaia Farmakologiia 56(4): 41-44

1993


ISSN/ISBN: 0869-2092
PMID: 8220015
Document Number: 420778
Scatchard's analysis was used to examine the specific binding of 3H-acetonide of triamcinolone (3H-AT) by Type II glucocorticoid receptors of cytosol from the liver of Wistar rats weighing 180-200 g. It was found that analgin in concentrations of 5.0 and 10.0 mM inhibited the density of glucocorticoid receptors and increase the dissociate rate constant of 3H-AT from the receptor and decreased 3H-AT elimination half-life from the receptor. Analgin in concentrations of 0.04, 0.08, 0.16, 0.31, 0.62, 1.25, and 2.50 mM lowered the association constant of the 3H-AT-receptor complex in proportion to the increase of analgin concentrations. Analgin was found to have uncompetitive effects followed by inhibition of the density of Type II glucocorticoid receptors.

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