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Analysis of the action of lidocaine on insect sodium channels.

Publication ,  Journal Article
Song, W; Silver, KS; Du, Y; Liu, Z; Dong, K
Published in: Insect biochemistry and molecular biology
January 2011

A new class of sodium channel blocker insecticides (SCBIs), which include indoxacarb, its active metabolite, DCJW, and metaflumizone, preferably block inactivated states of both insect and mammalian sodium channels in a manner similar to that by which local anesthetic (LA) drugs block mammalian sodium channels. A recent study showed that two residues in the cockroach sodium channel, F1817 and Y1824, corresponding to two key LA-interacting residues identified in mammalian sodium channels are not important for the action of SCBIs on insect sodium channels, suggesting unique interactions of SCBIs with insect sodium channels. However, the mechanism of action of LAs on insect sodium channels has not been investigated. In this study, we examined the effects of lidocaine on a cockroach sodium channel variant, BgNa(v)1-1a, and determined whether F1817 and Y1824 are also critical for the action of LAs on insect sodium channels. Lidocaine blocked BgNa(v)1-1a channels in the resting state with potency similar to that observed in mammalian sodium channels. Lidocaine also stabilized both fast-inactivated and slow-inactivated states of BgNa(v)1-1a channels, and caused a limited degree of use- and frequency-dependent block, major characteristics of LA action on mammalian sodium channels. Alanine substitutions of F1817 and Y1824 reduced the sensitivity of the BgNa(v)1-1a channel to the use-dependent block by lidocaine, but not to tonic blocking and inactivation stabilizing effects of lidocaine. Thus, similar to those on mammalian sodium channels, F1817 and Y1824 are important for the action of lidocaine on cockroach sodium channels. Our results suggest that the receptor sites for lidocaine and SCBIs are different on insect sodium channels.

Duke Scholars

Published In

Insect biochemistry and molecular biology

DOI

EISSN

1879-0240

ISSN

0965-1748

Publication Date

January 2011

Volume

41

Issue

1

Start / End Page

36 / 41

Related Subject Headings

  • Xenopus laevis
  • Sodium Channels
  • Sodium Channel Blockers
  • Patch-Clamp Techniques
  • Oocytes
  • Lidocaine
  • Kinetics
  • Ion Channel Gating
  • Insecticides
  • Insect Proteins
 

Citation

APA
Chicago
ICMJE
MLA
NLM
Song, W., Silver, K. S., Du, Y., Liu, Z., & Dong, K. (2011). Analysis of the action of lidocaine on insect sodium channels. Insect Biochemistry and Molecular Biology, 41(1), 36–41. https://doi.org/10.1016/j.ibmb.2010.09.010
Song, Weizhong, Kristopher S. Silver, Yuzhe Du, Zhiqi Liu, and Ke Dong. “Analysis of the action of lidocaine on insect sodium channels.Insect Biochemistry and Molecular Biology 41, no. 1 (January 2011): 36–41. https://doi.org/10.1016/j.ibmb.2010.09.010.
Song W, Silver KS, Du Y, Liu Z, Dong K. Analysis of the action of lidocaine on insect sodium channels. Insect biochemistry and molecular biology. 2011 Jan;41(1):36–41.
Song, Weizhong, et al. “Analysis of the action of lidocaine on insect sodium channels.Insect Biochemistry and Molecular Biology, vol. 41, no. 1, Jan. 2011, pp. 36–41. Epmc, doi:10.1016/j.ibmb.2010.09.010.
Song W, Silver KS, Du Y, Liu Z, Dong K. Analysis of the action of lidocaine on insect sodium channels. Insect biochemistry and molecular biology. 2011 Jan;41(1):36–41.
Journal cover image

Published In

Insect biochemistry and molecular biology

DOI

EISSN

1879-0240

ISSN

0965-1748

Publication Date

January 2011

Volume

41

Issue

1

Start / End Page

36 / 41

Related Subject Headings

  • Xenopus laevis
  • Sodium Channels
  • Sodium Channel Blockers
  • Patch-Clamp Techniques
  • Oocytes
  • Lidocaine
  • Kinetics
  • Ion Channel Gating
  • Insecticides
  • Insect Proteins