二苯氰胂对毒蕈碱性受体的抑制作用  

The antagonist effects of diphenylcyanoarsine on muscarinic receptors

作　　者：鹿晓晶[1] 王惠芳[1] 张瑞华[1] 李丽琴[1] 徐建富[1] 

机构地区：[1]北京防化研究院毒理学试验室,北京102205

出　　处：《毒理学杂志》2006年第1期19-21,共3页Journal of Toxicology

摘　　要：目的研究了日本在我国遗弃的化学武器———二苯氰胂(DC)对离体豚鼠回肠纵肌和毒蕈碱性受体的作用机制,为评估DC的毒理学作用及其对环境的影响提供依据。方法取豚鼠8只,分离豚鼠回肠纵肌16条,分4组,用累积给药法,从低到高分别给予不同浓度的DC,记录离体豚鼠回肠纵肌收缩的幅度,求出DC作用于离体回肠纵肌的EC50值,并通过DC与乙酰胆碱(AChR)的相互作用,研究DC的作用机制。在放射性配体-受体结合实验中,从10只大鼠大脑中提取受体,通过DC与[3H]QNB的竞争结合作用,研究了DC对毒蕈碱性受体的作用。结果DC可抑制离体豚鼠回肠纵肌的收缩作用,其对离体豚鼠回肠纵肌的EC50值为(7.335±2.377)×10-7mol/L,AChR可收缩离体豚鼠回肠,并可反转DC引起离体豚鼠回肠纵肌的舒张作用。在放射性配体-受体结合实验中,DC与毒蕈碱性受体结合的Ki值为(9.19±1.52)nmol/L,IC50值为(16.00±2.65)nmol/L。结论DC可作用于mAChR受体上,初步断定为AChR的拮抗剂。Objective To study the toxicological mechanism induced by diphenylcyanoarsine（DC）left in China by Japan during the Second World War,we investigated the effects on isolated musculus longitudinalis of ileum and muscarinic receptor in order to realize the toxic properties of DC and its influence on environments, Methods 16 strips of the musculus longitudinalis of ileum from 8 guinea pigs were isolated, divided into 4 groups, then administered different dosage of DC from low to high on musculus longitudinalis, recorded the contractive range and calculated the EC50 value of DC. We studied the reciprocities between DC and acetylcholine and realized the effective mechanism of DC. In the radioligand-receptor binding experiments, we extracted receptor from 10 rat＇s cerebra, then the competitive binding of DC and [^3H] QNB to the receptor was studies. Results DC could restrain the contractive effect on musculus longitudinalis of ileum. The EC50 value of DC on isolated musculus longitudinalis of ileum was（7.335 ± 2,377 ） ×10^- 7 mol/L. Causing the contraction of the isolated musculus longitudinalis of ileum, so acetylcholine could antagonize the effect of DC. In the radioligandreceptor binding experiments, the Ki value and IC50 value were （9.19 ± 1.52） and （ 16.130 ± 2.65） nmol/L respectively. Conclusion DC can bind to muscarinic receptor and is a antagonist of acetylcholine.

关 键 词：二苯氰胂 毒草碱性受体 豚鼠离体回肠纵肌实验 放射配体受体结合实验 

分 类 号：R99[医药卫生—毒理学]