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Molecular Mechanism of Action and Selectivity of Sodium Ch annel Blocker Insecticides.

Publication ,  Journal Article
Silver, K; Dong, K; Zhorov, BS
Published in: Current medicinal chemistry
January 2017

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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Published In

Current medicinal chemistry

DOI

EISSN

1875-533X

ISSN

0929-8673

Publication Date

January 2017

Volume

24

Issue

27

Start / End Page

2912 / 2924

Related Subject Headings

  • Xenopus
  • Voltage-Gated Sodium Channels
  • Sodium Channel Blockers
  • Semicarbazones
  • Oxazines
  • Oocytes
  • Medicinal & Biomolecular Chemistry
  • Insecticides
  • Humans
  • Animals
 

Citation

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Silver, K., Dong, K., & Zhorov, B. S. (2017). Molecular Mechanism of Action and Selectivity of Sodium Ch annel Blocker Insecticides. Current Medicinal Chemistry, 24(27), 2912–2924. https://doi.org/10.2174/0929867323666161216143844
Silver, Kristopher, Ke Dong, and Boris S. Zhorov. “Molecular Mechanism of Action and Selectivity of Sodium Ch annel Blocker Insecticides.Current Medicinal Chemistry 24, no. 27 (January 2017): 2912–24. https://doi.org/10.2174/0929867323666161216143844.
Silver K, Dong K, Zhorov BS. Molecular Mechanism of Action and Selectivity of Sodium Ch annel Blocker Insecticides. Current medicinal chemistry. 2017 Jan;24(27):2912–24.
Silver, Kristopher, et al. “Molecular Mechanism of Action and Selectivity of Sodium Ch annel Blocker Insecticides.Current Medicinal Chemistry, vol. 24, no. 27, Jan. 2017, pp. 2912–24. Epmc, doi:10.2174/0929867323666161216143844.
Silver K, Dong K, Zhorov BS. Molecular Mechanism of Action and Selectivity of Sodium Ch annel Blocker Insecticides. Current medicinal chemistry. 2017 Jan;24(27):2912–2924.

Published In

Current medicinal chemistry

DOI

EISSN

1875-533X

ISSN

0929-8673

Publication Date

January 2017

Volume

24

Issue

27

Start / End Page

2912 / 2924

Related Subject Headings

  • Xenopus
  • Voltage-Gated Sodium Channels
  • Sodium Channel Blockers
  • Semicarbazones
  • Oxazines
  • Oocytes
  • Medicinal & Biomolecular Chemistry
  • Insecticides
  • Humans
  • Animals