增效剂NIA16388对家蝇的毒理机制

以家蝇为材料,研究了增效剂ＮＩＡ１６３８８（简称ＮＩＡ）对其的毒理作用。结果表明,ＮＩＡ对家蝇具有相当高的毒性,这是ＮＩＡ对多个靶标位点综合作用的结果。ＮＩＡ可抑制羧酸酯酶的活性,Ｉ５０值为（２．４１±０．７５）×１０－６ｍｏｌ／Ｌ（α－ＮＡ）,（６．４９±２．０４）×１０－８ｍｏｌ／Ｌ（β－ＮＡ）;ＮＩＡ为４．２０×１０－４ｍｏｌ／Ｌ时,对多功能氧化酶的抑制率高达（９８．３５±２．４０）％。ＡＣｈＥ对ＮＩＡ十分敏感,Ｉ５０值为（２．２９±０．７９）×１０－７ｍｏｌ／Ｌ。ＮＩＡ对神经突触体ＡＴＰａｓｅ有一定的抑制作用。     

Quantitative structure-activity studies of substituted benzyl chrysanthemates: 1. Correlations between symptomatic and neurophysiological activities against American cockroaches

A number of substituted benzyl (1R)-trans-chrysanthemates and related compounds were synthesized. Their symptomatic activities in terms of levels which induce convulsions as well as cause death in American cockroaches were determined by injection with and without application of synergists as inhibitors of metabolism. The neuroexcitatory and neuroblocking activities were also determined in terms of minimum effective concentrations to induce repetitive train of impulses and conduction blockage, respectively, to central nerve cords excised from the cockroaches and immersed in Ringer's solution. Correlations between symptomatic and neurophysiological activities were analyzed quantitatively with the aid of molecular hydrophobicity parameter and regression analysis. Each symptomatic activity from which the effect of metabolism is eliminated was found to be analyzable by means of a linear combination of indices for two types of neurophysiological activity when the transport factor is separated by using the hydrophobicity parameter. A closer correlation was found between neuroblocking activity and the “convulsive” effect than between neuroexcitatory activity and the “convulsive” effect, whereas both neurophysiological effects operate together on the cockroaches resulting in paralysis and death.     

增效剂NIA16388对溴氰菊酯增效机理的研究

以抗溴氰菊酯品系家蝇(Del-R) 为试材,测定了NIA 对溴氰菊酯的增效作用,结果表明:NIA 对溴氰菊酯有极显著的增效作用。此后对NIA 的增效机理进行了研究,实验证明:NIA 可抑制家蝇体内羧酸酯酶的活性,I50值分别为2.14(±0.22)×10-7mo l·L-1(α-NA )和1.09(±0.39) ×10-9mol·L -1(β-NA ) ,N IA 为4.20×10- 4mol·L- 1时, 其对多功能氧化酶的抑制率达78.63(±0.13)%;此外,NIA 对神经靶标部位的AChE 也有抑制作用, I50值为2.37(±0169)×10- 5mo l·L - 1。几方面综合作用的结果, 使其表现出明显的增效效果。