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[肟类化合物的毒性及其对动物血液和肌神经突触中乙酰胆碱酯酶活性的影响]

[Toxicity of oximes and their effect on acetylcholinesterase activity in the blood and myoneural synapses of animals].

作者信息

Georgiev B, Khristoskova E

出版信息

Vet Med Nauki. 1978;15(2):108-15.

PMID:360596
Abstract

The effect was followed up of 2-PAM and Toxogonin (T), reactivators of choline esterase, at a single muscular application on the activity of acetylcholine esterase (ES 3.1.1.7) (ACE) of whole blood (WB) and the myoneural synapses (MS) of an interrib muscle. It was found that a species-specific effect was produced by T and 2-PAM on ACE of WB and MS in lambs and sheep. Optimal doses of 50 and 80 mg/kg led to a slight drop in the activity of ACE at the 2nd hour following injection, after which it rose gradually up to values that were higher than the initial ones for more than ten days. 100 and 200 mg/kg led to a more sensitive and long-term drop in the activity of ACE (up to 48h--72nd hour), after which it likewise rose above the initial value, and came back to normal on the 13th day. With lambs the reaction was analogous, though weaker. In rats and rabbits there was no change in the activity of ACE of WB and MS following the use of oximes. The optimal nontoxic and inductoenzyme rates of the two oximes for lambs and sheep proved to be about 50 mg/kg. It was established that both for rats and for sheep and lambs T was almost twice as toxic as 2-PAM. Intoxication with T was characterized by severe hemorrhagic and necrotic nephroso-nephritis, acute toxic dystrophy of the liver, and ulcerous, necrotic enteritis. 2-PAM was found to potentiate the toxic effect of T.

摘要

研究了胆碱酯酶复活剂2 - 解磷定(2 - PAM)和氯磷定(T)单次肌肉注射对全血(WB)乙酰胆碱酯酶(ES 3.1.1.7)(ACE)活性以及肋间肌肌神经突触(MS)的影响。结果发现,T和2 - PAM对羔羊和绵羊的全血和肌神经突触中的ACE产生了种属特异性效应。50和80mg/kg的最佳剂量在注射后第2小时导致ACE活性略有下降,之后逐渐上升,在十多天内升至高于初始值的水平。100和200mg/kg导致ACE活性更敏感且长期下降(直至48小时 - 72小时),之后同样升至初始值以上,并在第13天恢复正常。羔羊的反应类似,但较弱。在大鼠和兔子中,使用肟类药物后全血和肌神经突触中的ACE活性没有变化。事实证明,两种肟类药物对羔羊和绵羊的最佳无毒和诱导酶速率约为50mg/kg。已确定,对于大鼠以及绵羊和羔羊,T的毒性几乎是2 - PAM的两倍。T中毒的特征是严重的出血性和坏死性肾间质性肾炎、急性肝毒性营养不良以及溃疡性坏死性肠炎。发现2 - PAM可增强T的毒性作用。

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