4-(3-Cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone (ZK 62711): a potent inhibitor of adenosine cyclic 3',5'-monophosphate phosphodiesterases in homogenates and tissue slices from rat brain.

摘要: A new class of inhibitor phosphodiesterases is represented by 4-(3-cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone (ZK 62711). This compound enhances the magnitude accumulations cyclic 39,59-AMP elicited norepinephrine, isoproterenol, histamine, and adenosine in rat cerebral cortical slices veratridine cerebellar and, addition, increases basal levels AMP both slices. Increases intracellular brain ZK 62711 do not appear to involve enhanced "release" adenosine, since norepinephrine-elicited are increased presence exogenous deaminase. has little effect on GMP or In homogenates inhibits soluble particulate but less potent with respect phosphodiesterases. At low concentrations it 100 times more than a structurally related phosphodiesterase inhibitor, Ro 20-1724, calcium-dependent phosphodiesterase, similarly enhancing norepinephrine.