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预防梭曼中毒的新型模拟器:储存部位的结构特异性

New simulators in the prophylaxis against soman poisoning: structural specificity for the depot site(s).

作者信息

Van Helden H P, Benschop H P, Wolthuis O L

出版信息

J Pharm Pharmacol. 1984 May;36(5):305-8. doi: 10.1111/j.2042-7158.1984.tb04379.x.

DOI:10.1111/j.2042-7158.1984.tb04379.x
PMID:6145765
Abstract

The oxime HI-6 is effective as an antidote in the soman poisoned (6-8LD50) rat, however, successfully treated animals subsequently show a gradual relapse of signs of poisoning and eventually die after several hours. The relapse is caused by the reappearance of soman at specific sites, after having been elsewhere in the body. Diaphragms isolated from poisoned rats successfully treated with HI-6 also showed a 'secondary' relapse of poisoning. Eight compounds chemically related to soman-soman-simulators--have been tested as prophylactic agents, for their potency in preventing the reappearance of poisoning. The idea was that such compounds may block the non-synaptic binding sites for soman. Three of the 8 compounds proved very effective, which gave some insight into the chemical structure needed for this type of prophylactic action.

摘要

肟HI-6对梭曼中毒(6-8倍半数致死剂量)的大鼠有解毒作用,然而,成功治疗后的动物随后会逐渐出现中毒症状复发,最终在数小时后死亡。复发是由于梭曼在体内其他部位后,又在特定部位重新出现所致。从经HI-6成功治疗的中毒大鼠分离出的膈肌也出现了中毒的“二次”复发。已测试了8种与梭曼化学相关的化合物——梭曼模拟物——作为预防剂,看它们预防中毒症状复发的效力。其想法是这类化合物可能会阻断梭曼的非突触结合位点。8种化合物中有3种证明非常有效,这为这种预防作用所需化学结构提供了一些见解。

相似文献

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New simulators in the prophylaxis against soman poisoning: structural specificity for the depot site(s).预防梭曼中毒的新型模拟器:储存部位的结构特异性
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HI-6, an oxime which is an effective antidote of soman poisoning: a structure-activity study.HI-6,一种肟类化合物,是梭曼中毒的有效解毒剂:一项构效关系研究。
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Toxicology and pharmacology of bispyridium oximes--insight into the mechanism of action vs Soman poisoning in vivo.双吡啶肟类化合物的毒理学与药理学——对体内抗梭曼中毒作用机制的深入了解
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Effect of the bispyridinium oximes HGG12 and HGG42 and ganglion blocking agents on synaptic transmission and NAD(P)H-fluorescence in the superior cervical ganglion of the rat after Soman poisoning in vitro.在体外梭曼中毒后,双吡啶肟类化合物HGG12和HGG42以及神经节阻断剂对大鼠颈上神经节突触传递和NAD(P)H荧光的影响。
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Evidence for an intramuscular depot of the cholinesterase inhibitor soman in the rat.大鼠体内存在胆碱酯酶抑制剂梭曼的肌肉内储存库的证据。
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Cholinesterase and carboxylesterase activities in soman poisoned rats treated with bispyridinium mono-oximes HI-6 and HS-6.用双吡啶单肟类化合物HI-6和HS-6治疗的梭曼中毒大鼠的胆碱酯酶和羧酸酯酶活性
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HI6 as an antidote to soman poisoning in rhesus monkey respiratory muscles in-vitro.
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