Ilien B, Ruckstuhl M, Landry Y
J Pharmacol. 1982 Apr-Jun;13(2):307-16.
Two cyclic nucleotide phosphodiesterases sensitive to calmodulin were partially purified from bovine brain and bovine aorta. The enzyme from bovine brain exhibited the properties of the "high Km phosphodiesterase", with a higher Km for cyclic AMP than for cyclic GMP. The enzyme from bovine aorta hydrolyzed both cyclic AMP and cyclic GMP with similar kinetics. The hydrolysis of cyclic AMP by the brain enzyme was selectively inhibited by papaverine and 2' deoxy cyclic AMP. The hydrolysis of cyclic GMP by this enzyme was selectively inhibited by cyclic IMP, 2' deoxy cyclic GMP, 1-methyl-3-isobutyl-xanthine, ICI 74917 and M & B 22948. All these inhibitors were identically potent on the hydrolysis of both substrates by the aorta enzyme. Ro-20 1724, an imidazolidinone, and ZK 62711, a pyrrolidone, two compounds known to be potent inhibitors of cyclic AMP phosphodiesterase insensitive to calmodulin, were inefficient inhibitors of both calmodulin-sensitive phosphodiesterases.
从牛脑和牛主动脉中部分纯化出两种对钙调蛋白敏感的环核苷酸磷酸二酯酶。牛脑来源的酶表现出“高Km磷酸二酯酶”的特性，对环磷酸腺苷（cAMP）的Km值高于环磷酸鸟苷（cGMP）。牛主动脉来源的酶以相似的动力学水解cAMP和cGMP。脑来源的酶对cAMP的水解被罂粟碱和2'-脱氧环磷酸腺苷选择性抑制。该酶对cGMP的水解被环磷酸肌苷（cIMP）、2'-脱氧环磷酸鸟苷、1-甲基-3-异丁基黄嘌呤、ICI 74917和M&B 22948选择性抑制。所有这些抑制剂对主动脉来源的酶水解两种底物的效力相同。Ro-20 1724（一种咪唑烷酮）和ZK 62711（一种吡咯烷酮），这两种已知对钙调蛋白不敏感的环磷酸腺苷磷酸二酯酶有强效抑制作用的化合物，对两种钙调蛋白敏感的磷酸二酯酶都是低效抑制剂。
