Rudakova E V, Boltneva N P, Makhaeva G F
Laboratory of Molecular Toxicology, Institute of Physiologically Active Substances, Russian Academy of Sciences, Chernogolovka, Moscow Region, Russia.
Bull Exp Biol Med. 2011 Nov;152(1):73-5. doi: 10.1007/s10517-011-1457-y.
Acetylcholinesterase, butyrylcholinesterase, carboxylesterase, and paraoxonase activities in human, mouse, and rat blood were measured. The proportions of these enzymes activities differed significantly. In humans, the most significant were cholinesterase activities, while in rats and mice the contribution of carboxylesterase activity was the greatest. High arylesterase activity of paraoxonase was observed in all cases. Species-specific differences should be taken into consideration when carrying out preclinical trials on rodents for optimization of the pharmacokinetic characteristics of drugs containing complex ester groups.
测定了人、小鼠和大鼠血液中乙酰胆碱酯酶、丁酰胆碱酯酶、羧酸酯酶和对氧磷酶的活性。这些酶活性的比例差异显著。在人类中,胆碱酯酶活性最为显著,而在大鼠和小鼠中,羧酸酯酶活性的贡献最大。在所有情况下均观察到对氧磷酶的高芳基酯酶活性。在对啮齿动物进行临床前试验以优化含有复杂酯基药物的药代动力学特性时,应考虑物种特异性差异。