[The effect of analgin on glucocorticoid receptors].
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.
Golikov
P P
PP
Nikolaeva
N Iu
NIu
D000818:Animals; D003600:Cytosol / Q000187:drug effects / Q000378:metabolism; D004177:Dipyrone / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005260:Female; D066298:In Vitro Techniques; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D011965:Receptors, Glucocorticoid / Q000187:drug effects* / Q000378:metabolism; D014222:Triamcinolone Acetonide / Q000493:pharmacokinetics; D014316:Tritium
D011965:Receptors, Glucocorticoid; D014316:Tritium; D004177:Dipyrone; D014222:Triamcinolone Acetonide
Vliianie anal'gina na gliukokortikoidnye retseptory.