New GABA/Glutamate Receptor Target for [3H]Isoxazoline Insecticide
The highly effective and selective isoxazoline insecticide A1443 is known to potently displace [3H]ethynylbicycloorthobenzoate ([3H]EBOB) binding to house fly head membranes with an IC50 of 0.2 nM in a manner characteristic of GABA-gated chloride channel antagonists. To further define its mode of ac...
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| Veröffentlicht in: | Chemical research in toxicology 2013-04, Vol.26 (4), p.514-516 |
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| creator | García-Reynaga, Pablo Zhao, Chunqing Sarpong, Richmond Casida, John E |
| description | The highly effective and selective isoxazoline insecticide A1443 is known to potently displace [3H]ethynylbicycloorthobenzoate ([3H]EBOB) binding to house fly head membranes with an IC50 of 0.2 nM in a manner characteristic of GABA-gated chloride channel antagonists. To further define its mode of action, we prepared phenyl-labeled [3H]A1443 as described with a specific activity of 14 Ci/mmol. This new radioligand with an apparent IC50 of about 0.4 nM is poorly displaced by most insecticides acting at the [3H]EBOB site. Interestingly, the isoxazoline binding site is directly coupled to the avermectin GABA/glutamate chloride channel activator site. These findings revive interest in the insect GABA/glutamate receptor as an insecticide target. |
| doi_str_mv | 10.1021/tx400055p |
| format | Article |
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To further define its mode of action, we prepared phenyl-labeled [3H]A1443 as described with a specific activity of 14 Ci/mmol. This new radioligand with an apparent IC50 of about 0.4 nM is poorly displaced by most insecticides acting at the [3H]EBOB site. Interestingly, the isoxazoline binding site is directly coupled to the avermectin GABA/glutamate chloride channel activator site. 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These findings revive interest in the insect GABA/glutamate receptor as an insecticide target.</description><subject>Animals</subject><subject>Binding Sites</subject><subject>Houseflies</subject><subject>Insect Proteins - metabolism</subject><subject>Insecticides - metabolism</subject><subject>Isoxazoles - metabolism</subject><subject>Receptors, GABA - metabolism</subject><subject>Receptors, Glutamate - metabolism</subject><issn>0893-228X</issn><issn>1520-5010</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNptkFtLwzAUgIMoOi8P_gHpi6AP1VzX9UXYROdAFERBEAmn6YlWumYmqbdfb2U6FHzKgXx85_ARss3oAaOcHcY3SSlVarZEekxxmirK6DLp0UEuUs4Ht2tkPYQnSlmHZ6tkjQvZVzTjPTK6wNdkPBwND8d1G2EKEZMrNDiLzifX4B8wJrYb78TZ_SS4N_hwddVgMmkCmliZqsRNsmKhDrj1_W6Qm9OT6-Oz9PxyPDkenqegqIypBWGLvA_AJRU2lyo30C9RyhxlgcYUImdWZANlSxxwymWeoQUsoJTCsqIQG-Ro7p21xRRLg030UOuZr6bg37WDSv_9aapH_eBetMgEkyzrBHvfAu-eWwxRT6tgsK6hQdcG3aWTIld9zjp0f44a70LwaBdrGNVfzfWiecfu_L5rQf5E7oDdOQAm6CfX-qbL9I_oE2YCibI</recordid><startdate>20130415</startdate><enddate>20130415</enddate><creator>García-Reynaga, Pablo</creator><creator>Zhao, Chunqing</creator><creator>Sarpong, Richmond</creator><creator>Casida, John E</creator><general>American Chemical Society</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>7TK</scope><scope>7U7</scope><scope>C1K</scope><scope>5PM</scope></search><sort><creationdate>20130415</creationdate><title>New GABA/Glutamate Receptor Target for [3H]Isoxazoline Insecticide</title><author>García-Reynaga, Pablo ; Zhao, Chunqing ; Sarpong, Richmond ; Casida, John E</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-a504t-fa3fb96aa2403f9459ca6de449e4beccb391f3785fde8202497efaebad43f1bb3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>Animals</topic><topic>Binding Sites</topic><topic>Houseflies</topic><topic>Insect Proteins - metabolism</topic><topic>Insecticides - metabolism</topic><topic>Isoxazoles - metabolism</topic><topic>Receptors, GABA - metabolism</topic><topic>Receptors, Glutamate - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>García-Reynaga, Pablo</creatorcontrib><creatorcontrib>Zhao, Chunqing</creatorcontrib><creatorcontrib>Sarpong, Richmond</creatorcontrib><creatorcontrib>Casida, John E</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><collection>Toxicology Abstracts</collection><collection>Environmental Sciences and Pollution Management</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Chemical research in toxicology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>García-Reynaga, Pablo</au><au>Zhao, Chunqing</au><au>Sarpong, Richmond</au><au>Casida, John E</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>New GABA/Glutamate Receptor Target for [3H]Isoxazoline Insecticide</atitle><jtitle>Chemical research in toxicology</jtitle><addtitle>Chem. Res. Toxicol</addtitle><date>2013-04-15</date><risdate>2013</risdate><volume>26</volume><issue>4</issue><spage>514</spage><epage>516</epage><pages>514-516</pages><issn>0893-228X</issn><eissn>1520-5010</eissn><abstract>The highly effective and selective isoxazoline insecticide A1443 is known to potently displace [3H]ethynylbicycloorthobenzoate ([3H]EBOB) binding to house fly head membranes with an IC50 of 0.2 nM in a manner characteristic of GABA-gated chloride channel antagonists. To further define its mode of action, we prepared phenyl-labeled [3H]A1443 as described with a specific activity of 14 Ci/mmol. This new radioligand with an apparent IC50 of about 0.4 nM is poorly displaced by most insecticides acting at the [3H]EBOB site. Interestingly, the isoxazoline binding site is directly coupled to the avermectin GABA/glutamate chloride channel activator site. 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| fulltext | fulltext |
| identifier | ISSN: 0893-228X |
| ispartof | Chemical research in toxicology, 2013-04, Vol.26 (4), p.514-516 |
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| language | eng |
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| source | MEDLINE; ACS Publications |
| subjects | Animals Binding Sites Houseflies Insect Proteins - metabolism Insecticides - metabolism Isoxazoles - metabolism Receptors, GABA - metabolism Receptors, Glutamate - metabolism |
| title | New GABA/Glutamate Receptor Target for [3H]Isoxazoline Insecticide |
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