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卤化物对大鼠肝脏碳酸酐酶的抑制作用。

Inhibition of carbonic anhydrases of rat liver by halides.

作者信息

Garg L C

出版信息

J Pharmacol Exp Ther. 1977 Feb;200(2):434-8.

PMID:839447
Abstract

The hepatic carbonic anhydrases from male rat are known to differ from those of female rat in being resistant to inhibition by sulfonamides. In the present work the inhibition of carbonic anhydrases from livers of male and female rats by chloride and iodide was studied in the CO2 hydration reaction. The hepatic carbonic anhydrases from male rats were found to be more susceptible to inhibition by halides (I50 and Cl- = 7-15 mM, and I- = 0.7-1.5 mM). On the other hand, the hepatic carbonic anhydrases from female rats were less susceptible to inhibition by halides (I50 for Cl- = 150-250 mM and for I- = 3-10 mM). The presence of bicarbonate increased I50 of both Cl- and I- for liver isoenzymes of both male and female rats by about 2- to 20-fold. The differential susceptibility of carbonic anhydrases from livers of male and female rats to inhibition by halides was in contrast to their susceptibility to inhibition by sulfonamides.

摘要

已知雄性大鼠肝脏中的碳酸酐酶与雌性大鼠的不同,对磺胺类药物的抑制具有抗性。在本研究中,研究了氯化物和碘化物在二氧化碳水合反应中对雄性和雌性大鼠肝脏碳酸酐酶的抑制作用。发现雄性大鼠肝脏中的碳酸酐酶更容易受到卤化物的抑制(氯离子的半数抑制浓度为7 - 15 mM,碘离子为0.7 - 1.5 mM)。另一方面,雌性大鼠肝脏中的碳酸酐酶对卤化物的抑制较不敏感(氯离子的半数抑制浓度为150 - 250 mM,碘离子为3 - 10 mM)。碳酸氢盐的存在使雄性和雌性大鼠肝脏同工酶的氯离子和碘离子的半数抑制浓度增加了约2至20倍。雄性和雌性大鼠肝脏碳酸酐酶对卤化物抑制的敏感性差异与它们对磺胺类药物抑制的敏感性相反。

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