Possible participation of glucocorticoid in elevation of 3',5'-cyclic AMP levels through inhibition of cyclic AMP phosphodiesterase.
Administration of prednisolone and cholate to rats elevated levels of cAMP (adenosine 3',5'-cyclic monophosphate) by 1.5- to 2.0-fold. Compounds such as prednisolone, hydrocortisone, cholate, and deoxycholate were found to be potent inhibitors of partially purified cAMP phosphodiesterase prepared from rat liver. Kinetic analysis showed that the prednisolone inhibition was noncompetitive with a Ki of 8.9 x 10(-4) M. These results suggest that in addition to increasing DNA-dependent RNA polymerase activity in vivo, a large application of glucocorticoid may incur elevation of intracellular cAMP levels.
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D000818:Animals; D002793:Cholic Acids / Q000494:pharmacology; D000242:Cyclic AMP / Q000032:analysis*; D003840:Deoxycholic Acid / Q000494:pharmacology; D005938:Glucocorticoids / Q000494:pharmacology*; D006854:Hydrocortisone / Q000494:pharmacology; D008099:Liver / Q000032:analysis / Q000187:drug effects* / Q000201:enzymology; D008297:Male; D011239:Prednisolone / Q000494:pharmacology; D051381:Rats
D002793:Cholic Acids; D005938:Glucocorticoids; D003840:Deoxycholic Acid; D011239:Prednisolone; D000242:Cyclic AMP; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D006854:Hydrocortisone