[The activation of specific type-III glucocorticoid receptors by pyrazolone series preparations].
Experiments were conducted on intact and adrenalectomized male Wistar rats (weighing 180-200 g) with labelled corticosterone of high specific activity to study the effect of analgin and aminopyrine on the level of type-III glucocorticoid receptors in the liver. Analgin and aminopyrine in doses of 10(-2) and 10(-3) increase the specific binding of labelled corticosterone by type-III glucocorticoid receptors of the hepatic cytosol and by blood plasma transcortin in modelled experiments. The effect of the agents depends on the dose. Intravenous administration of 140 mg/100 g of analgin to intact rats and intraperitoneal injection of an equal dose of analgin to adrenalectomized rats also increases the specific binding of labelled corticosterone by type-III glucocorticoid receptors of the hepatic cytosol. The importance of the revealed effect of agents of the pyrazolone series in stress regulation is discussed.
Golikov
P P
PP
Nikolaeva
N Iu
NIu
Kladiev
A A
AA
D000315:Adrenalectomy; D000632:Aminopyrine / Q000494:pharmacology; D000818:Animals; D003345:Corticosterone / Q000378:metabolism*; D003600:Cytosol / Q000187:drug effects / Q000378:metabolism; D004177:Dipyrone / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D008297:Male; D011720:Pyrazoles / Q000494:pharmacology*; D047069:Pyrazolones; D051381:Rats; D011919:Rats, Inbred Strains; D011965:Receptors, Glucocorticoid / Q000187:drug effects* / Q000378:metabolism; D011987:Receptors, Steroid; D014156:Transcortin / Q000378:metabolism; D014316:Tritium
D011720:Pyrazoles; D047069:Pyrazolones; D011965:Receptors, Glucocorticoid; D011987:Receptors, Steroid; C024357:corticosterone receptor; D000632:Aminopyrine; D014316:Tritium; C038362:pyrazolone; D004177:Dipyrone; D014156:Transcortin; D003345:Corticosterone
Aktivatsiia spetsificheskikh gliukokortikoidnykh retseptorov III tipa preparatami pirazolonovogo riada.