Abstract
Sodium channel blocker insecticides (SCBIs) are a relatively new class of insecticides that are represented by two commercially registered compounds, indoxacarb and metaflumizone. SCBIs, like pyrethroids and DDT, target voltage-gated sodium channels (VGSCs) to intoxicate insects. In contrast to pyrethroids, however, SCBIs inhibit VGSCs at a distinct receptor site that overlaps those of therapeutic inhibitors of sodium channels, such as local anesthetics, anticonvulsants and antiarrhythmics. This review will recount the development of the SCBI insecticide class from its roots as chitin synthesis inhibitors, discuss the symptoms of poisoning and evidence supporting inhibition of VGSCs as their mechanism of action, describe the current model for SCBI-induced inhibition of VGSCs, present a model for the receptor for SCBIs on VGSCs, and highlight differences between data collected from mammalian and insect experimental models.
Keywords: Voltage-gated sodium channels, sodium channel blocker insecticides, metaflumizone, indoxacarb, statedependent channel block, insecticide receptors.
Current Medicinal Chemistry
Title:Molecular Mechanism of Action and Selectivity of Sodium Ch annel Blocker Insecticides
Volume: 24 Issue: 27
Author(s): Kristopher Silver*, Ke Dong and Boris S. Zhorov
Affiliation:
- Department of Entomology, 1603 Old Claflin Place, 123 Waters Hall, Kansas State University, Manhattan, KS 66506,United States
Keywords: Voltage-gated sodium channels, sodium channel blocker insecticides, metaflumizone, indoxacarb, statedependent channel block, insecticide receptors.
Abstract: Sodium channel blocker insecticides (SCBIs) are a relatively new class of insecticides that are represented by two commercially registered compounds, indoxacarb and metaflumizone. SCBIs, like pyrethroids and DDT, target voltage-gated sodium channels (VGSCs) to intoxicate insects. In contrast to pyrethroids, however, SCBIs inhibit VGSCs at a distinct receptor site that overlaps those of therapeutic inhibitors of sodium channels, such as local anesthetics, anticonvulsants and antiarrhythmics. This review will recount the development of the SCBI insecticide class from its roots as chitin synthesis inhibitors, discuss the symptoms of poisoning and evidence supporting inhibition of VGSCs as their mechanism of action, describe the current model for SCBI-induced inhibition of VGSCs, present a model for the receptor for SCBIs on VGSCs, and highlight differences between data collected from mammalian and insect experimental models.
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Cite this article as:
Silver Kristopher*, Dong Ke and Zhorov S. Boris, Molecular Mechanism of Action and Selectivity of Sodium Ch annel Blocker Insecticides, Current Medicinal Chemistry 2017; 24 (27) . https://dx.doi.org/10.2174/0929867323666161216143844
DOI https://dx.doi.org/10.2174/0929867323666161216143844 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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