Loomis C W, Brien J F
Can J Physiol Pharmacol. 1983 Apr;61(4):431-5. doi: 10.1139/y83-065.
Acute, oral administration of 7.0 mg/kg calcium carbimide (calcium cyanamide) to rats, 2 h before sacrifice, produced complete inhibition of hepatic, low-Km (less than 1 microM acetaldehyde) mitochondrial and cytosolic aldehyde dehydrogenase enzymes and significantly inhibited high-Km (approximately 1 mM acetaldehyde) mitochondrial, cytosolic, and microsomal aldehyde dehydrogenase isozymes. Calcium carbimide had no effect on several other hepatic enzyme activities including mitochondrial glutamate dehydrogenase and monoamine oxidase, cytosolic alcohol dehydrogenase, microsomal NADPH-cytochrome c reductase, benzo[a]pyrene hydroxylase and aminopyrine N-demethylase activities, and microsomal cytochrome P-450 content. It is concluded that calcium carbimide is a more specific inhibitor of hepatic aldehyde dehydrogenase enzymes than disulfiram.
在处死大鼠前2小时,经口给大鼠急性注射7.0毫克/千克的卡巴咪嗪(氰胺化钙),可完全抑制肝脏中低Km(小于1微摩尔乙醛)的线粒体和胞质醛脱氢酶,并显著抑制高Km(约1毫摩尔乙醛)的线粒体、胞质和微粒体醛脱氢酶同工酶。卡巴咪嗪对其他几种肝脏酶活性没有影响,包括线粒体谷氨酸脱氢酶和单胺氧化酶、胞质乙醇脱氢酶、微粒体NADPH-细胞色素c还原酶、苯并[a]芘羟化酶和氨基比林N-脱甲基酶活性,以及微粒体细胞色素P-450含量。结论是,与双硫仑相比,卡巴咪嗪是一种对肝脏醛脱氢酶更具特异性的抑制剂。