• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>RSC Advances >Recent developments on oximes to improve the blood brain barrier penetration for the treatment of organophosphorus poisoning: a review
【24h】

Recent developments on oximes to improve the blood brain barrier penetration for the treatment of organophosphorus poisoning: a review

机译：氧化母近期发展，提高血脑屏障渗透治疗有机磷中毒：综述

获取原文
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Organophosphorus (OP) compounds are highly toxic synthetic compounds which have been used as pesticides and developed as warfare nerve agents. They represent a threat to both military and civilian populations. OP pesticides affect the nervous system and are thought to have caused at least 5 million deaths since their discovery in the 1930s. At present the treatment of OP nerve agent poisoning commonly involves the use of parenteral oximes. However, the blood brain barrier (BBB) remains a challenge in the delivery of oximes to the central nervous system (CNS). This is because almost all macromolecule drugs (including oximes) fail to pass through the BBB to reach the CNS structures. The presence of a permanent cationic charge in oximes has made these compounds inefficient in crossing the BBB. Thus, oximes are unable to reactivate acetylcholinesterase (AChE) in the CNS. Using current structural and mechanistic understanding of the BBB under both physiological and pathological conditions, it becomes possible to design delivery systems for oximes and other drugs that are able to cross the BBB effectively. This review summarises the recent strategies in the development of oximes which are capable of crossing the BBB to treat OP poisoning. Several new developments using oximes are reviewed along with their advantages and disadvantages. This review could be beneficial for future directions in the development of oxime and other drug delivery systems into the CNS.
机译：有机磷（OP）化合物是高度毒性的合成化合物，已被用作农药，并作为战争神经试剂发展。它们代表对军事和民用人口的威胁。 OP农药影响神经系统，并被认为自20世纪30年代发现以来造成了至少500万人死亡。目前op神经药物中毒的治疗通常涉及使用肠胃外肟。然而，血脑屏障（BBB）仍然是在向中枢神经系统（CNS）的氧化时呈挑战。这是因为几乎所有的大分子药物（包括氧化肟）都不能通过BBB来达到CNS结构。在肟中存在永久阳离子电荷使这些化合物在交叉BBB中效率低下。因此，肟不能在CNS中重新激活乙酰胆碱酯酶（ACHE）。在生理和病理条件下，利用对BBB对BBB的电流结构和机械理解，可以设计肟和其他能够有效交叉BBB的其他药物的递送系统。本综述总结了最近开发氧化肟的策略，其能够穿越BBB治疗OP中毒。使用氧化跳的几个新的发展以及它们的优缺点。本综述可能有利于未来在肟和其他药物递送系统发展到CNS中的方向。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号