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氯苯甘醚与二价金属离子和磷酸二酯酶的相互作用。

Interactions of chlorphenesin and divalent metal ions with phosphodiesterase.

作者信息

Edelson J, McMullen J P

出版信息

Arch Int Pharmacodyn Ther. 1976 Sep;223(1):24-33.

PMID:187130
Abstract

Chlorphenesin inhibition of the hydrolysis of cyclic AMP by guinea-pig lung phosphodiesterase was reversed by the addition of exogenous magnesium ions. Chlorphenesin and theophylline inhibition of this enzyme was shown to be noncompetitive when the substrate concentration was low. Kinetic studies of the inhibition of beef heart phosphodiesterase by chlorphenesin and theophylline indicated that the substrate concentration was a factor in determining whether inhibition was competitive or noncompetitive. Calcium, cobalt and copper ions were inhibitory to guinea-pig lung phosphodiesterase. The inhibition due to chlorphenesin was partially reversed by low (40 mM or less) concentrations of barium ions; high concentrations of barium ions, or manganese ions, were inhibitory. The concentration of the divalent cation did not affect the type of inhibition that was observed.

摘要

添加外源镁离子可逆转氯苯甘醚对豚鼠肺磷酸二酯酶水解环磷酸腺苷的抑制作用。当底物浓度较低时,氯苯甘醚和茶碱对该酶的抑制作用表现为非竞争性。对氯苯甘醚和茶碱抑制牛心磷酸二酯酶的动力学研究表明,底物浓度是决定抑制作用是竞争性还是非竞争性的一个因素。钙、钴和铜离子对豚鼠肺磷酸二酯酶有抑制作用。低浓度(40 mM或更低)的钡离子可部分逆转氯苯甘醚引起的抑制作用;高浓度的钡离子或锰离子具有抑制作用。二价阳离子的浓度不影响所观察到的抑制类型。

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