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| 宾赛克嗪拮抗M和N胆碱受体的特征及其抗胆碱酯酶抑制剂的毒性效应 | |
| 引用本文： | 崔文玉,张雁芳,潘志远,赵想弟,龙超良,汪海.宾赛克嗪拮抗M和N胆碱受体的特征及其抗胆碱酯酶抑制剂的毒性效应[J].中国药理学通报,2011,27(7):915-921. |
| 作者姓名： | 崔文玉 张雁芳 潘志远 赵想弟 龙超良 汪海 |
| 作者单位： | 1. 军事医学科学院卫生学环境医学研究所,北京,100850 2. 北京赛德维康医药研究院,北京,100039 3. 军事医学科学院卫生学环境医学研究所,北京,100850;北京赛德维康医药研究院,北京,100039 |
| 基金项目： | 国家重大新药创制科技重大专项资助项目 |
| 摘 要： | 目的评价宾赛克嗪(benthiactzine)对胆碱受体功能拮抗作用及其对有机磷农药中毒的抗毒效应,并与阿托品比较。方法①以烟碱诱发小鼠惊厥,离体豚鼠回肠收缩为评价中枢和外周神经元N受体功能的指标;以槟榔碱诱发小鼠震颤为评价中枢M受体功能的指标;以槟榔碱和毛果芸香碱诱发小鼠流涎,乙酰胆碱和氧化震颤素诱发回肠收缩为评价外周M受体功能的指标;并在烟碱和毛果芸香碱联用诱发混合性震颤模型上,研究药物的药理学特点。②在DDVP染毒小鼠模型上研究药物的抗毒效应(PR值)。结果①宾赛克嗪抗槟榔碱致小鼠中枢性震颤的ED50±L95为(0.31±0.06)mg.kg-1,中枢抗M作用比阿托品(1.33±0.17)mg.kg-1强3.3倍。②宾赛克嗪抗槟榔碱和毛果芸香碱诱发小鼠流涎的ED50±L95分别为(0.38±0.09)mg.kg-1和(5.57±1.30)mg.kg-1,而阿托品分别为(0.17±0.03)mg.kg-1和(0.46±0.18)mg.kg-1,宾赛克嗪的外周抗M作用弱于阿托品。③宾赛克嗪抗烟碱诱发惊厥的ED50±L95为(2.87±0.76)mg.kg-1,具有较强的中枢抗N作用。④宾赛克嗪抗烟碱诱发回肠收缩的IC50±L95为(1.1±0.18)μmol.L-1,比阿托品(13.84±1.68)μmol.L-1强约13倍,说明宾赛克嗪具有外周神经元N受体拮抗作用。⑤宾赛克嗪抗毛果芸香碱和烟碱联用诱发小鼠震颤的ED50±L95为(2.64±0.35)mg.kg-1,比阿托品(4.95±0.65)mg.kg-1强约1倍。⑥宾赛克嗪和阿托品抗DDVP致死作用的ED50±L95分别为(2.87±0.40)mg.kg-1和(6.78±3.92)mg.kg-1;宾赛克嗪10 mg.kg-1可使小鼠抗DDVP中毒的PR值提高16.84倍,而阿托品仅能提高0.81倍。结论宾赛克嗪中枢抗M作用强于阿托品,外周抗M作用弱于阿托品,并具有中枢和外周神经元N受体拮抗作用;宾赛克嗪对敌敌畏中毒小鼠的抗毒效应明显强于阿托品。 |
| 关 键 词： | 胆碱酯酶抑制剂 有机磷农药中毒 M受体 N受体 宾赛克嗪 阿托品 |
Pharmacological characteristics of benthiactzine's antagonism on cholinergic receptors and its antidotal effects against cholinesterase inhibitors poisoning |
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| CUI Wen-yu,ZHANG Yan-fang,PAN Zhi-yuan,ZHAO Xiang-di,LONG Chao-liang,WANG Hai.Pharmacological characteristics of benthiactzine's antagonism on cholinergic receptors and its antidotal effects against cholinesterase inhibitors poisoning[J].Chinese Pharmacological Bulletin,2011,27(7):915-921. | |
| Authors: | CUI Wen-yu ZHANG Yan-fang PAN Zhi-yuan ZHAO Xiang-di LONG Chao-liang WANG Hai |
| Institution: | CUI Wen-yu1,ZHANG Yan-fang1,PAN Zhi-yuan1,ZHAO Xiang-di2,LONG Chao-liang1,WANG Hai1,2 (1.Institute of Health and Environmental Medicine,Academy of Military Medical Sciences,Beijing 100850,China,2.Thadweik Academy of Medicine,Beijing 100039,China) |
| Abstract: | Aim To investigate the pharmacological characteristics of benthiactzine's antagonism on cholinergic receptors activities and to evaluate the antidotal effects of benthiactzine against ChEI poisoning,which were compared with the effects of atropine.Methods The convulsions in mice and the construction of isolated guinea pig ileum induced by nicotine were used to assess the effects of benthiactzine on central and peripheral nicotinic receptors.The central tremor and peripheral salivation caused by arecoline,th... |
| Keywords: | acetylcholinesterase inhibitors organophosphorus pesticide poisoning muscarinic receptor nicotinic receptor benthiactzine atropine |
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