Ehrich M, Correll L, Strait J, McCain W, Wilcke J
Virginia-Maryland Regional College of Veterinary Medicine, Blacksburg, Virginia 24061.
J Toxicol Environ Health. 1992 Aug;36(4):411-23. doi: 10.1080/15287399209531648.
Carbaryl, a carbamate insecticide, exerts its toxic effect in animals by inhibiting the activity of neural acetylcholinesterase. Differences in sensitivity of this enzyme to inhibition were studied after intraperitoneal administration to chickens and rats. A dose of 900 mg/kg to chickens and 70 mg/kg to rats caused equivalent inhibition of brain cholinesterase activities (57% +/- 6 and 47% +/- 4, respectively) 60 min after administration, which was the time of maximal cholinergic signs. Signs of toxicity (salivation, respiratory distress, muscle tremors and weakness) were more pronounced in rats than in chickens when brain acetylcholinesterase was inhibited to the same extent in both species. Carboxylesterase activities in brain, liver, and plasma were also inhibited 60 min after administration of carbaryl to chickens and rats. Activities of enzymes associated with hepatic microsomes were unaffected. Specific activities of brain esterases, including acetylcholinesterase, carboxylesterase and neurotoxic esterase, were higher in untreated chickens than in untreated rats. Specific activities of liver esterases (carboxylesterase, A-esterase) were, however, 4- and 10-fold lower in untreated chickens than in untreated rats. Total clearance of carbaryl in the chicken, determined after intravenous administration of 5 mg/kg, was 0.26 +/- 0.02 l/kg/min. This value is 5.7 times higher than that reported for the rat, indicating that the relatively lower activities of esterases in the liver of chickens did not affect the clearance of this chemical in the avian species.
西维因是一种氨基甲酸酯类杀虫剂,它通过抑制神经乙酰胆碱酯酶的活性在动物体内发挥毒性作用。在给鸡和大鼠腹腔注射后,研究了这种酶对抑制作用的敏感性差异。给药后60分钟,给鸡900毫克/千克、给大鼠70毫克/千克的剂量对脑胆碱酯酶活性产生了等效抑制(分别为57%±6和47%±4),这是胆碱能症状最明显的时间。当两个物种的脑乙酰胆碱酯酶被抑制到相同程度时,大鼠的中毒症状(流涎、呼吸窘迫、肌肉震颤和无力)比鸡更明显。给鸡和大鼠注射西维因60分钟后,脑、肝和血浆中的羧酸酯酶活性也受到抑制。与肝微粒体相关的酶的活性未受影响。未处理的鸡脑中包括乙酰胆碱酯酶、羧酸酯酶和神经毒性酯酶在内的酯酶的比活性高于未处理的大鼠。然而,未处理的鸡肝酯酶(羧酸酯酶、A酯酶)的比活性比未处理的大鼠低4倍和10倍。静脉注射5毫克/千克后测定的鸡体内西维因的总清除率为0.26±0.02升/千克/分钟。这个值比报道的大鼠的值高5.7倍,表明鸡肝脏中酯酶活性相对较低并不影响该化学物质在鸟类中的清除。