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在袋狸大鼠中,毒鼠强(N-3-吡啶基甲基-N'-对硝基苯基脲)对血清乙酰胆碱酯酶(E.C.3.1.1.7)的非竞争性抑制作用。

Non-competitive inhibition of serum acetylcholinesterase (E.C.3.1.1.7) by vacor (N-3-pyridyl methyl-N'-P-nitrophenyl urea) in bandicoot rats.

作者信息

Devi S V, Krishnamoorthy R V

出版信息

Indian J Physiol Pharmacol. 1979 Oct-Dec;23(4):285-90.

PMID:528034
Abstract

Single dose (1 mg/rat) administration of VACOR (N-3-pyridyl methyl-N'-nitrophenyl urea) produced significant paralytic symptoms in rats. Such rats which lived for one week were sacrificed and serum AChE was extracted and purified by Sephadex column chromatography. The serum enzyme from the normal rats showed the existence of two isozymes on polyacrylamide gels which could be resolved through column chromatography. Both the isozymes showed non-competitive inhibition with VACOR in vitro; but to a varied degree. The ACh concentration increased by 70-75% in serum and 95-100% in erythrocytes of the poisoned rats. VACOR thus affects ACh hydrolysis thereby causing an accumulation of ACh in the serum of poisoned rats.

摘要

给大鼠单次注射1毫克/只的灭鼠灵(N-3-吡啶基甲基-N'-硝基苯基脲)会使其出现明显的麻痹症状。存活一周的此类大鼠被处死,血清乙酰胆碱酯酶通过葡聚糖凝胶柱色谱法提取和纯化。正常大鼠的血清酶在聚丙烯酰胺凝胶上显示存在两种同工酶,这两种同工酶可通过柱色谱法分离。两种同工酶在体外均对灭鼠灵表现出非竞争性抑制作用,但程度不同。中毒大鼠血清中的乙酰胆碱浓度增加了70 - 75%,红细胞中的乙酰胆碱浓度增加了95 - 100%。因此,灭鼠灵影响乙酰胆碱的水解,从而导致中毒大鼠血清中乙酰胆碱的积累。

相似文献

1
Non-competitive inhibition of serum acetylcholinesterase (E.C.3.1.1.7) by vacor (N-3-pyridyl methyl-N'-P-nitrophenyl urea) in bandicoot rats.在袋狸大鼠中,毒鼠强(N-3-吡啶基甲基-N'-对硝基苯基脲)对血清乙酰胆碱酯酶(E.C.3.1.1.7)的非竞争性抑制作用。
Indian J Physiol Pharmacol. 1979 Oct-Dec;23(4):285-90.
2
Vacor inhibits insulin release from islets in vitro.灭鼠优在体外抑制胰岛释放胰岛素。
J Endocrinol Invest. 1989 Apr;12(4):273-5. doi: 10.1007/BF03349985.
3
Accidental ingestion of Vacor rodenticide: the symptoms and sequelae in a 25-month-old child.意外摄入灭鼠灵:一名25个月大儿童的症状及后遗症
Am J Dis Child. 1980 Feb;134(2):161-4.
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Inhibition of mitochondrial complex I may account for IDDM induced by intoxication with the rodenticide Vacor.线粒体复合体I的抑制可能是由灭鼠剂Vacor中毒诱发的胰岛素依赖型糖尿病的原因。
Diabetes. 1996 Nov;45(11):1531-4. doi: 10.2337/diab.45.11.1531.
5
Diabetes mellitus and neuropathy following Vacor ingestion in man.人类摄入灭鼠灵后的糖尿病和神经病变。
Arch Intern Med. 1979 Feb;139(2):185-7.
6
Adenosine A1 receptor agonist N6-cyclopentyladenosine affects the inactivation of acetylcholinesterase in blood and brain by sarin.腺苷A1受体激动剂N6-环戊基腺苷影响沙林对血液和大脑中乙酰胆碱酯酶的灭活作用。
J Pharmacol Exp Ther. 2003 Mar;304(3):1307-13. doi: 10.1124/jpet.102.044644.
7
Protective effects of a series of new pyridinium derivatives against inhibition of acetylcholinesterase by fluostigmine.一系列新型吡啶鎓衍生物对氟斯的明抑制乙酰胆碱酯酶的保护作用。
Pharmazie. 1978 Feb-Mar;33(2-3):120-1.
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Electrocardiographic changes on sublethal poisoning of Vacor and Silmurin to Bandicota bengalensis.杀鼠灵和灭鼠优对板齿鼠亚致死中毒时的心电图变化
Indian J Physiol Pharmacol. 1981 Jan-Mar;25(1):48-52.
9
Bait shyness towards zinc phosphide & vacor in the larger bandicoot rat Bandicota indica (Bechstein).大长爪鼠(Bandicota indica,贝希斯坦)对磷化锌和毒鼠强的诱饵回避行为
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[Comparative characteristics of acetylcholinesterase preparations from human erythrocytes with varying degrees of purity].[不同纯度人红细胞乙酰胆碱酯酶制剂的比较特征]
Prikl Biokhim Mikrobiol. 1978 Jan-Feb;14(1):78-84.