[Modulation of glucocorticoid receptor interaction with non-steroidal drugs].
The Scatchard analysis of the specific binding of triamcinolone 3H-acetonide (TA-3HA) to Type II glucocorticoid receptors of cytosol from the liver of female Wistar rats weighing 180-200 g has shown that emoxipin at concentrations of 1 and 2 mM and analgin at concentrations of 5 and 10 mM reduce the density of glucocorticoid receptors and the association constant of a hormone-receptor complex. Analgin, 5 mM, increases the dissociation velocity constant of TA-3HA 5 times the effect of unlabeled triamcinolone acetonide. Emoxipin, 1 mM, produces the same effect on the receptor dissociation velocity constant of TA-3HA as the unlabeled triamcinolone acetonide. The Berke analysis has established that emoxipin and analgin reduce glucocorticoid receptor interactions by uncompetitive inhibition.
Golikov
P P
PP
Nikolaeva
N Iu
NIu
D000818:Animals; D004177:Dipyrone / Q000378:metabolism*; D005260:Female; D010847:Picolines / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D011965:Receptors, Glucocorticoid / Q000378:metabolism*
D010847:Picolines; D011965:Receptors, Glucocorticoid; D004177:Dipyrone; C009820:6-methyl-2-ethyl-3-hydroxypyridine
Moduliatsiia gliukokortikoid-retseptornogo vzaimodeĭstviia nesteroidnymi lekarstvennymi sredstvami.