Wu D, Costa L G, Murphy S D
Department of Environmental Health, University of Washington.
Hua Xi Yi Ke Da Xue Xue Bao. 1990 Mar;21(1):17-21.
Chlordimeform (CDM) and Amitraz (AMZ) are two formamidine pesticides. CDM and AMZ inhibited the binding of 3H-Clonidine, 3H-Yohimbine to Alpha 2-adrenoreceptor of rat forebrain tissue in vitro with IC50 values of 62-68 mumol/L (CDM) and 95-110 mumol/L (AMZ). In vivo the administration of CDM and AMZ by ip showed the effect of inhibition on the binding and significant correlation of dose-effect r = 0.995 (CDM), 0.884 (AMZ). Time course test indicated that the lasting inhibition effect of CDM following exposure was shorter than AMZ. Similar results were observed with plasma in vitro. Comparing inhibition effects on rat forebrain tissue, directly induced by CDM and AMZ at different doses, with the results from the plasma of treated rats in vitro, there was a significant correlation r = 0.973 (CDM), 0.909 (AMZ). It showed that the inhibition effect of both CDM and AMZ was linked to the concentration of compounds chemical and their metabolites in blood. Time course and washing test indicated that the inhibition effect by CDM and AMZ was reversible.
杀虫脒（CDM）和双甲脒（AMZ）是两种脒类农药。CDM和AMZ在体外抑制3H-可乐定、3H-育亨宾与大鼠前脑组织α2-肾上腺素能受体的结合，IC50值分别为62 - 68μmol/L（CDM）和95 - 110μmol/L（AMZ）。在体内，腹腔注射CDM和AMZ显示出对结合的抑制作用，且剂量效应呈显著相关，r = 0.995（CDM），0.884（AMZ）。时间进程试验表明，暴露后CDM的持续抑制作用比AMZ短。体外血浆试验也观察到类似结果。比较不同剂量的CDM和AMZ对大鼠前脑组织的直接抑制作用与体外处理大鼠血浆的结果，存在显著相关性，r = 0.973（CDM）, 0.909（AMZ）。这表明CDM和AMZ的抑制作用均与血液中化合物及其代谢产物的浓度有关。时间进程和洗脱试验表明，CDM和AMZ的抑制作用是可逆的。
