Capuzzo A, Biondi C, Borasio P G, Ferretti M E, Fabbri E
Neurochem Res. 1986 Oct;11(10):1425-37. doi: 10.1007/BF00966222.
Adenosine 3',5'-cyclic monophosphate (cAMP) phosphodiesterase activity in crude guinea-pig superior cervical ganglion homogenates was assayed under a variety of experimental conditions. Two forms of cAMP phosphodiesterase were found, one with high and the other with low affinity for the substrate. The Km values were about 1 and 110 microM respectively. Imidazole slightly but constantly stimulated the former enzyme form over a wide range of concentrations and 1-methyl-3-isobutylxanthine was a weak competitive inhibitor with a Ki value of 90 microM. Low affinity cAMP phosphodiesterase activity was increased by calmodulin and Ca2+. This stimulation was not observed in the presence of trifluoperazine, a specific inhibitor of calmodulin. On the other hand, neither [D-Ala2]met-enkephalinamide nor prostaglandin E2, alone or in combination, influenced high affinity cAMP phosphodiesterase.
在多种实验条件下,对豚鼠颈上神经节粗制匀浆中的3',5'-环磷酸腺苷(cAMP)磷酸二酯酶活性进行了测定。发现了两种形式的cAMP磷酸二酯酶,一种对底物具有高亲和力,另一种具有低亲和力。Km值分别约为1和110微摩尔。咪唑在很宽的浓度范围内对前一种酶形式有轻微但持续的刺激作用,1-甲基-3-异丁基黄嘌呤是一种弱竞争性抑制剂,Ki值为90微摩尔。低亲和力的cAMP磷酸二酯酶活性可被钙调蛋白和Ca2+增强。在钙调蛋白的特异性抑制剂三氟拉嗪存在的情况下未观察到这种刺激作用。另一方面,单独或联合使用的[D-Ala2]甲硫脑啡肽酰胺和前列腺素E2均不影响高亲和力的cAMP磷酸二酯酶。