【摘要】 十四种消草磷结构类似物与经苯巴比妥预处理大鼠肝匀浆S9悬液一起温育,在有NADPH存在时,可不同程度地使P450失活.若温育10 min后P450丢失量用Y表示,化合物的疏水性和电性分别用P_gc和μ_gc表示,可建立如下相关性: logY=4.106logP_gc-0.575(logP_gc)²-5.822 （n=14,r=0.954,s=0.054）;logY=3.678 logP_gc-0.520(logP_gc)²-0.037μ_gc-4.877 （n=14,r=0.965,S=0.049） 上述两方程表明,消草磷同类物体外使P450失活的能力与其疏水性呈良好的抛物线型相关,化合物的电性对此能力也有影响,但贡献较小.更多还原

【Abstract】 In the presence of NADPH regenerating system,14 amiprophos analogues incubated with hepatic S9 fraction of the phenobarbital-pretreated rats might inactivate cytochrome P450 in different degrees.If the loss of cytochrome P4SO was expressed as Y(% of control value)and Pgc andμgc as hydrophobic and electronic parameters of these tested compounds respectively,the following regression equations could be established:logY=4.1061ogPgc-0.575(logPgc)2-5.822(n=14,r=0.954,s=0.054)logY=3.678logPgc-0.520(logPgc)2-0.037μgc-4.877(n=14,r=0.965,s=0.049)The two equations indicate that the relationship between hydrophobic parameters of amiprophos analogues and their ability to inactivate cytochrome P450 in vitro appeared to be parabolic type with a quite high regression coeffient.Although the electronic parameters of them(μgc of the substrates)also affected their inactivating ability,but the contribution was much smaller than that of the hydrophobic property.更多还原