• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

使用肟K027在体外对乙酰胆碱酯酶进行再激活。

In vitro reactivation of acetylcholinesterase using the oxime K027.

作者信息

Kuca Kamil, Kassa Jirí

机构信息

Purkyne Military Medical Academy, Department of Toxicology, PO Box 35/T, 500 01 Hradec Králové, Czech Republic.

出版信息

Vet Hum Toxicol. 2004 Feb;46(1):15-8.

PMID:14748409
Abstract

The ability of a new bisquaternary oxime, K027 (1-[4-hydroxyiminomethylpyridinium]-3-[carbamoylpyridinium] propane dibromide), to reactivate the enzyme acetylcholinesterase (AChE) inhibited by the nerve agents Tabun, sarin and VX was evaluated. Its reactivation potency was compared to the AChE reactivators pralidoxime (2-PAM), obidoxime and HI-6; K027 seems a good reactivator of organophosphates-inhibited AChE. Its reactivation potency is lower compared to the other oximes for reactivation of sarin-inhibited AChE, but it is sufficient to significantly increase the activity of sarin-inhibited AChE. Its reactivation ability is comparable to obidoxime for reactivation of VX- and tabun-inhibited AChE and is higher than the reactivation potency of HI-6, for tabun-inhibited AChE. HI-6 is currently regarded the most promising reactivator of organophosphates-inhibited AChE.

摘要

对一种新型双季铵肟K027(1-[4-羟基亚胺甲基吡啶鎓]-3-[氨基甲酰基吡啶鎓]丙烷二溴化物)使被神经毒剂塔崩、沙林和维埃克斯抑制的乙酰胆碱酯酶(AChE)重新活化的能力进行了评估。将其重新活化效力与AChE重新活化剂氯解磷定(2-PAM)、双复磷和HI-6进行了比较;K027似乎是有机磷酸酯抑制的AChE的良好重新活化剂。在重新活化沙林抑制的AChE方面,其重新活化效力低于其他肟类,但足以显著提高沙林抑制的AChE的活性。在重新活化维埃克斯和塔崩抑制的AChE方面,其重新活化能力与双复磷相当,在重新活化塔崩抑制的AChE方面,其重新活化效力高于HI-6。HI-6目前被认为是有机磷酸酯抑制的AChE最有前景的重新活化剂。

相似文献

1
In vitro reactivation of acetylcholinesterase using the oxime K027.使用肟K027在体外对乙酰胆碱酯酶进行再激活。
Vet Hum Toxicol. 2004 Feb;46(1):15-8.
2
In vitro reactivation potency of acetylcholinesterase reactivators--K074 and K075--to reactivate tabun-inhibited human brain cholinesterases.乙酰胆碱酯酶复活剂——K074和K075——对塔崩抑制的人脑胆碱酯酶的体外复活效力。
Neurotox Res. 2007 Feb;11(2):101-6. doi: 10.1007/BF03033389.
3
In vitro reactivation of tabun-inhibited acetylcholinesterase using new oximes--K027, K005, K033 and K048.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。
Cent Eur J Public Health. 2004 Mar;12 Suppl:S59-61.
4
New quaternary pyridine aldoximes as casual antidotes against nerve agents intoxications.新型季铵吡啶肟作为神经性毒剂中毒的通用解毒剂。
Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2005 Jun;149(1):75-82. doi: 10.5507/bp.2005.008.
5
Currently used cholinesterase reactivators against nerve agent intoxication: comparison of their effectivity in vitro.目前用于对抗神经毒剂中毒的胆碱酯酶复活剂:它们在体外的有效性比较。
Drug Chem Toxicol. 2007;30(1):31-40. doi: 10.1080/01480540601017637.
6
Reactivating potency of obidoxime, pralidoxime, HI 6 and HLö 7 in human erythrocyte acetylcholinesterase inhibited by highly toxic organophosphorus compounds.高毒性有机磷化合物抑制人红细胞乙酰胆碱酯酶后,氯解磷定、解磷定、HI 6和HLö 7的复活效力
Arch Toxicol. 1998 Mar;72(4):237-43. doi: 10.1007/s002040050495.
7
Reactivation of sarin-inhibited pig brain acetylcholinesterase using oxime antidotes.使用肟类解毒剂使沙林抑制的猪脑乙酰胆碱酯酶重新激活。
J Med Toxicol. 2006 Dec;2(4):141-6. doi: 10.1007/BF03161181.
8
A comparison of the efficacy of a bispyridinium oxime--1,4-bis-(2-hydroxyiminomethylpyridinium) butane dibromide and currently used oximes to reactivate sarin, tabun or cyclosarin-inhibited acetylcholinesterase by in vitro methods.通过体外方法比较双吡啶肟——1,4 - 双(2 - 羟基亚氨基甲基吡啶)丁烷二溴化物与目前使用的肟类药物对沙林、塔崩或环沙林抑制的乙酰胆碱酯酶的复活效果。
Pharmazie. 2004 Oct;59(10):795-8.
9
In vitro and in vivo evaluation of pyridinium oximes: mode of interaction with acetylcholinesterase, effect on tabun- and soman-poisoned mice and their cytotoxicity.吡啶肟类化合物的体外和体内评价:与乙酰胆碱酯酶的相互作用模式、对塔崩和梭曼中毒小鼠的影响及其细胞毒性。
Toxicology. 2006 Feb 15;219(1-3):85-96. doi: 10.1016/j.tox.2005.11.003. Epub 2005 Dec 5.
10
A comparison of the potency of the oxime HLö-7 and currently used oximes (HI-6, pralidoxime, obidoxime) to reactivate nerve agent-inhibited rat brain acetylcholinesterase by in vitro methods.通过体外方法比较肟类化合物HLö-7与目前使用的肟类化合物(HI-6、解磷定、双复磷)对神经毒剂抑制的大鼠脑乙酰胆碱酯酶的重活化能力。
Acta Medica (Hradec Kralove). 2005;48(2):81-6.

引用本文的文献

1
Experimental and Established Oximes as Pretreatment before Acute Exposure to Azinphos-Methyl.实验性和已建立肟类化合物作为急性接触甲拌磷前的预处理。
Int J Mol Sci. 2021 Mar 17;22(6):3072. doi: 10.3390/ijms22063072.
2
Combined Pre- and Posttreatment of Paraoxon Exposure.联合使用对氧磷酶暴露前和暴露后的治疗。
Molecules. 2020 Mar 27;25(7):1521. doi: 10.3390/molecules25071521.
3
The Experimental Oxime K027-A Promising Protector From Organophosphate Pesticide Poisoning. A Review Comparing K027, K048, Pralidoxime, and Obidoxime.
实验性肟类化合物K027——有机磷农药中毒的一种有前景的保护剂。K027、K048、解磷定和双复磷的比较综述
Front Neurosci. 2019 May 22;13:427. doi: 10.3389/fnins.2019.00427. eCollection 2019.
4
A newly developed oxime K203 is the most effective reactivator of tabun-inhibited acetylcholinesterase.新研发的肟类化合物K203是对塔崩抑制的乙酰胆碱酯酶最有效的重活化剂。
BMC Pharmacol Toxicol. 2018 Feb 21;19(1):8. doi: 10.1186/s40360-018-0196-3.
5
Reactivation of sarin-inhibited pig brain acetylcholinesterase using oxime antidotes.使用肟类解毒剂使沙林抑制的猪脑乙酰胆碱酯酶重新激活。
J Med Toxicol. 2006 Dec;2(4):141-6. doi: 10.1007/BF03161181.
6
Targeted synthesis of 1-(4-hydroxyiminomethylpyridinium)-3-pyridiniumpropane dibromide--a new nerve agent reactivator.新型神经毒剂重活化剂1-(4-羟基亚胺甲基吡啶鎓)-3-吡啶鎓丙烷二溴化物的靶向合成
Molecules. 2007 Aug 20;12(8):1964-72. doi: 10.3390/12081964.
7
Two step synthesis of a non-symmetric acetylcholinesterase reactivator.非对称乙酰胆碱酯酶复活剂的两步合成法。
Molecules. 2007 Aug 7;12(8):1755-61. doi: 10.3390/12081755.
8
The influence of oxime and anticholinergic drug selection on the potency of antidotal treatment to counteract acute toxic effects of tabun in mice.肟类和抗胆碱能药物的选择对小鼠抗塔崩急性毒性解毒治疗效力的影响。
Neurotox Res. 2006 Jan;9(1):59-62. doi: 10.1007/BF03033308.