Inhibition of the activation of the rat liver cytosolic glucocorticoid receptor by Li+.
By the use of aqueous two-phase partitioning and DNA-Sepharose chromatography, Li+ has been found to cause a partial inhibition of the activation of the rat liver glucocorticoid receptor in vitro. During incubations of cytosol with 0.4 M KCl at 0 degrees C, the LiCl-concentration giving half-maximal effect is approx. 1 mM; at higher temperatures, the receptor is less susceptible to the effect of LiCl. Na+ counteracts the effect of Li+, the LiCl-concentration giving half-maximal effect in 0.4 M NaCl being at least 20-fold higher than that in 0.4 M KCl. These findings are best explained by an ion-binding mechanism, Li+ and Na+ competing for binding, but only the binding of Li+ leading to activation inhibition.
D000818:Animals; D003600:Cytosol / Q000378:metabolism; D008094:Lithium / Q000494:pharmacology*; D008099:Liver / Q000187:drug effects / Q000378:metabolism*; D051381:Rats; D011965:Receptors, Glucocorticoid / Q000187:drug effects* / Q000378:metabolism; D011987:Receptors, Steroid / Q000187:drug effects*
D011965:Receptors, Glucocorticoid; D011987:Receptors, Steroid; D008094:Lithium