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采用高效液相色谱法 ,测定血清和脑组织匀浆中的肟硫磷 ,揭示其经口染毒 SD大鼠体内的毒物代谢动力学过程 ;以血清丁酰胆碱酯酶 (BCh E)和脑组织乙酰胆碱酯酶 (ACh E)的抑制率及一氧化氮合酶 (NOS)活性为毒效应指标 ,阐明肟硫磷的毒效动力学特征 .给大鼠 ig肟硫磷 2 75mg·kg-1后 ,血清毒物浓度 -时间曲线符合一级吸收一室开放模型 ,ka= 1 .87h-1,Tp=1 .2 6h,Cmax=1 .90 mg· L-1.ACh E抑制效应与血清肟硫磷浓度之间呈逆时针滞后环 .脑组织中 NOS活性随时间进程的异常波动 ,提示 NO参与产生非胆碱能神经毒作用 . BCh E抑制以后不能迅速自动恢复 ,所致酶的“老化”,可能是产生胆碱能效应的直接证据
The contents of oxime, thiophosin in serum and brain homogenates were determined by high performance liquid chromatography (HPLC), revealing the toxicokinetic process in SD rats after oral administration. The serum butyrylcholinesterase (BChE) and The inhibition rate of acetylcholinesterase (ACh E) and the activity of nitric oxide synthase (NOS) in brain tissue were the indicators of toxic effect, and the pharmacodynamic characteristics of oxime were elucidated.Ganoxifene 2 75 mg · kg- 1, the concentration-time curve of serum poisons conformed to the first-order absorption one-compartment open model with ka = 1.87h-1, Tp = 1.26h, Cmax = 1.90 mg · L-1.ACh E inhibitory effect and serum The concentration of oxime was between the anti-clockwise lag ring.NOS activity in brain tissue abnormal fluctuations over time, suggesting that NO involved in the production of non-cholinergic neurotoxicity.CBCh E inhibition can not be quickly restored automatically, resulting in enzyme “ Aging, ”may be direct evidence of cholinergic effects