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.
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.
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。
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