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使用新型肟类化合物(K027、K005、K033和K048)对塔崩抑制的乙酰胆碱酯酶进行体外复活研究。

In vitro reactivation of tabun-inhibited acetylcholinesterase using new oximes--K027, K005, K033 and K048.

作者信息

Kuca K, Cabal J

机构信息

Department of Toxicology, Purkynĕ Medical Military Academy, Hradec Králové, Czech Republic.

出版信息

Cent Eur J Public Health. 2004 Mar;12 Suppl:S59-61.

Abstract

Four new AChE oximes for reactivation of acetylcholinesterase inhibited with tabun - K027 [1-(4-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium) propane dibromide], K005 [1,3-bis(2-hydroxyiminomethylpyridinium) propane dibromide], K033 [1,4-bis(2-hydroxyiminomethylpyridinium) butane dibromide] and K048 [1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium) butane dibromide] were prepared. Their efficacies to reactivate tabun-inhibited acetylcholinesterase were studied and compared with the currently used acetylcholinesterase reactivators (pralidoxime, obidoxime and HI-6). Reactivator K048 seems to be promising reactivator of tabun-inhibited AChE. Its reactivation potency is significantly higher than the efficacy of HI-6 and pralidoxime, and comparable with the potency of the obidoxime at human relevant doses.

摘要

制备了四种用于使被塔崩抑制的乙酰胆碱酯酶重新活化的新型乙酰胆碱酯酶肟类化合物——K027 [1-(4-羟基亚胺甲基吡啶鎓)-3-(4-氨甲酰基吡啶鎓)丙烷二溴化物]、K005 [1,3-双(2-羟基亚胺甲基吡啶鎓)丙烷二溴化物]、K033 [1,4-双(2-羟基亚胺甲基吡啶鎓)丁烷二溴化物]和K048 [1-(4-羟基亚胺甲基吡啶鎓)-4-(4-氨甲酰基吡啶鎓)丁烷二溴化物]。研究了它们使被塔崩抑制的乙酰胆碱酯酶重新活化的效果,并与目前使用的乙酰胆碱酯酶重新活化剂(解磷定、双复磷和HI-6)进行了比较。重新活化剂K048似乎是一种有前景的使被塔崩抑制的乙酰胆碱酯酶重新活化的试剂。其重新活化效力明显高于HI-6和解磷定的效果,在人体相关剂量下与双复磷的效力相当。

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