Bispyridinium Oximes As Antidotal Treatment of Cyclosarin Poisoning—In Vitro and In Vivo Testing
The mechanism of intoxication with organophosphorus compounds, including highly toxic nerve agents and less toxic pesticides, is based on the formation of irreversibly inhibited acetylcholinesterase, which causes cumulation of neuromediator acetylcholine in synaptic clefts and subsequent overstimula...
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| Veröffentlicht in: | International journal of toxicology 2005-11, Vol.24 (6), p.399-402 |
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| creator | Bartosova, Lucie Kuca, Kamil Jun, Daniel Kunesova, Gabriela |
| description | The mechanism of intoxication with organophosphorus compounds, including highly toxic nerve agents and less toxic pesticides, is based on the formation of irreversibly inhibited acetylcholinesterase, which causes cumulation of neuromediator acetylcholine in synaptic clefts and subsequent overstimulation of cholinergic receptors, that is followed by a generalized cholinergic crisis. Nerve agent poisoning is conventionally treated using a combination of a cholinolytic (atropine mostly) to counteract the accumulation of acetylcholine and acetylcholinesterase reactivators (pralidoxime or obidoxime) to reactivate inhibited acetylcholinesterase. In this study of cyclosarin poisoning treatment, oximes of different chemical structures (obidoxime, HI-6, BI-6, and HS-6) were tested in vitro on rat brain acetylcholinesterase (enzyme source: rat brain homogenate), and afterwards, they were tested in vivo in equimolar doses, in mice and rats. The HI-6 oxime appeared to be the most effective oxime in vitro and in vivo. |
| doi_str_mv | 10.1080/10915810500366567 |
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Nerve agent poisoning is conventionally treated using a combination of a cholinolytic (atropine mostly) to counteract the accumulation of acetylcholine and acetylcholinesterase reactivators (pralidoxime or obidoxime) to reactivate inhibited acetylcholinesterase. In this study of cyclosarin poisoning treatment, oximes of different chemical structures (obidoxime, HI-6, BI-6, and HS-6) were tested in vitro on rat brain acetylcholinesterase (enzyme source: rat brain homogenate), and afterwards, they were tested in vivo in equimolar doses, in mice and rats. 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Nerve agent poisoning is conventionally treated using a combination of a cholinolytic (atropine mostly) to counteract the accumulation of acetylcholine and acetylcholinesterase reactivators (pralidoxime or obidoxime) to reactivate inhibited acetylcholinesterase. In this study of cyclosarin poisoning treatment, oximes of different chemical structures (obidoxime, HI-6, BI-6, and HS-6) were tested in vitro on rat brain acetylcholinesterase (enzyme source: rat brain homogenate), and afterwards, they were tested in vivo in equimolar doses, in mice and rats. The HI-6 oxime appeared to be the most effective oxime in vitro and in vivo.</description><subject>Animals</subject><subject>Antidotes - pharmacology</subject><subject>Antidotes - therapeutic use</subject><subject>Atropine - therapeutic use</subject><subject>Brain - drug effects</subject><subject>Brain - enzymology</subject><subject>Cholinesterase Inhibitors - toxicity</subject><subject>Cholinesterase Reactivators - pharmacology</subject><subject>Cholinesterase Reactivators - therapeutic use</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Evaluation, Preclinical</subject><subject>Enzyme Inhibitors - toxicity</subject><subject>Female</subject><subject>In Vitro Techniques</subject><subject>Kinetics</subject><subject>Lethal Dose 50</subject><subject>Mice</subject><subject>Muscarinic Antagonists - therapeutic use</subject><subject>Obidoxime Chloride - pharmacology</subject><subject>Obidoxime Chloride - therapeutic use</subject><subject>Organophosphorus Compounds - toxicity</subject><subject>Oximes - pharmacology</subject><subject>Oximes - therapeutic use</subject><subject>Pyridinium Compounds - pharmacology</subject><subject>Pyridinium Compounds - therapeutic use</subject><subject>Rats</subject><subject>Rats, Wistar</subject><issn>1091-5818</issn><issn>1092-874X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kM1KAzEQx4Mofj-AF8nJ2-pkNx_boxY_CoV6qOJtSbNJSdlNarIr9uZD-IQ-ibEteBBkAjOZ-c0_5I_QGYFLAiVcERgQVhJgAAXnjIsddJh6eVYK-rK7rkmWgPIAHcW4AAAuGNlHB4QXgxT5IZrd2LhcBVtbZ_sWT95tqyO-Tsd1tvadbPA0aNm12nXYGzxcqcZHGazDj95G76ybf318jhx-tl3wWLoary9vHk917NL4BO0Z2UR9us3H6Onudjp8yMaT-9HwepwpSvIuE4ZQoYAXKjdSUaDMCDlgMhcMaF7OKFHKaMVJWRgQkoOZ1bokojC8JFzp4hhdbHSXwb_26e2qtVHpppFO-z5WOTBKWUETSDagCj7GoE21DLaVYVURqH6Mrf4Ym3bOt-L9rNX178bWyQRcboAo57pa-D649Nl_FL8B3mOBdg</recordid><startdate>200511</startdate><enddate>200511</enddate><creator>Bartosova, Lucie</creator><creator>Kuca, Kamil</creator><creator>Jun, Daniel</creator><creator>Kunesova, Gabriela</creator><general>SAGE Publications</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7U7</scope><scope>C1K</scope></search><sort><creationdate>200511</creationdate><title>Bispyridinium Oximes As Antidotal Treatment of Cyclosarin Poisoning—In Vitro and In Vivo Testing</title><author>Bartosova, Lucie ; Kuca, Kamil ; Jun, Daniel ; Kunesova, Gabriela</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c412t-7f147c063c2fac4045f7a95a2750428b41ccfec6183f07a60fbde8173f6816ce3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2005</creationdate><topic>Animals</topic><topic>Antidotes - pharmacology</topic><topic>Antidotes - therapeutic use</topic><topic>Atropine - therapeutic use</topic><topic>Brain - drug effects</topic><topic>Brain - enzymology</topic><topic>Cholinesterase Inhibitors - toxicity</topic><topic>Cholinesterase Reactivators - pharmacology</topic><topic>Cholinesterase Reactivators - therapeutic use</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug Evaluation, Preclinical</topic><topic>Enzyme Inhibitors - toxicity</topic><topic>Female</topic><topic>In Vitro Techniques</topic><topic>Kinetics</topic><topic>Lethal Dose 50</topic><topic>Mice</topic><topic>Muscarinic Antagonists - therapeutic use</topic><topic>Obidoxime Chloride - pharmacology</topic><topic>Obidoxime Chloride - therapeutic use</topic><topic>Organophosphorus Compounds - toxicity</topic><topic>Oximes - pharmacology</topic><topic>Oximes - therapeutic use</topic><topic>Pyridinium Compounds - pharmacology</topic><topic>Pyridinium Compounds - therapeutic use</topic><topic>Rats</topic><topic>Rats, Wistar</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bartosova, Lucie</creatorcontrib><creatorcontrib>Kuca, Kamil</creatorcontrib><creatorcontrib>Jun, Daniel</creatorcontrib><creatorcontrib>Kunesova, Gabriela</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Toxicology Abstracts</collection><collection>Environmental Sciences and Pollution Management</collection><jtitle>International journal of toxicology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Bartosova, Lucie</au><au>Kuca, Kamil</au><au>Jun, Daniel</au><au>Kunesova, Gabriela</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Bispyridinium Oximes As Antidotal Treatment of Cyclosarin Poisoning—In Vitro and In Vivo Testing</atitle><jtitle>International journal of toxicology</jtitle><addtitle>SPIJT</addtitle><date>2005-11</date><risdate>2005</risdate><volume>24</volume><issue>6</issue><spage>399</spage><epage>402</epage><pages>399-402</pages><issn>1091-5818</issn><eissn>1092-874X</eissn><abstract>The mechanism of intoxication with organophosphorus compounds, including highly toxic nerve agents and less toxic pesticides, is based on the formation of irreversibly inhibited acetylcholinesterase, which causes cumulation of neuromediator acetylcholine in synaptic clefts and subsequent overstimulation of cholinergic receptors, that is followed by a generalized cholinergic crisis. Nerve agent poisoning is conventionally treated using a combination of a cholinolytic (atropine mostly) to counteract the accumulation of acetylcholine and acetylcholinesterase reactivators (pralidoxime or obidoxime) to reactivate inhibited acetylcholinesterase. In this study of cyclosarin poisoning treatment, oximes of different chemical structures (obidoxime, HI-6, BI-6, and HS-6) were tested in vitro on rat brain acetylcholinesterase (enzyme source: rat brain homogenate), and afterwards, they were tested in vivo in equimolar doses, in mice and rats. The HI-6 oxime appeared to be the most effective oxime in vitro and in vivo.</abstract><cop>Los Angeles, CA</cop><pub>SAGE Publications</pub><pmid>16393932</pmid><doi>10.1080/10915810500366567</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Animals Antidotes - pharmacology Antidotes - therapeutic use Atropine - therapeutic use Brain - drug effects Brain - enzymology Cholinesterase Inhibitors - toxicity Cholinesterase Reactivators - pharmacology Cholinesterase Reactivators - therapeutic use Dose-Response Relationship, Drug Drug Evaluation, Preclinical Enzyme Inhibitors - toxicity Female In Vitro Techniques Kinetics Lethal Dose 50 Mice Muscarinic Antagonists - therapeutic use Obidoxime Chloride - pharmacology Obidoxime Chloride - therapeutic use Organophosphorus Compounds - toxicity Oximes - pharmacology Oximes - therapeutic use Pyridinium Compounds - pharmacology Pyridinium Compounds - therapeutic use Rats Rats, Wistar |
| title | Bispyridinium Oximes As Antidotal Treatment of Cyclosarin Poisoning—In Vitro and In Vivo Testing |
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