Skip to main content

Agents Affecting Sodium Channels

  • Chapter
  • 455 Accesses

Abstract

Voltage sensitive sodium channels are widely recognized as the site of action for two classes of insecticides, the diphenylethanes (e.g., DDT and analogs) and the pyrethroids. Diphenylethane insecticides have not been used in significant quantity in the United States for more than two decades, but pyrethroids are one of the most important and widely used classes of insecticides. This chapter considers the actions of pyrethroids on voltage sensitive sodium channels and other putative sites of action and assesses the significance of those effects in determining the toxic actions of these compounds.

This is a preview of subscription content, log in via an institution.

Buying options

Chapter
USD   29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD   189.00
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD   249.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD   249.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Learn about institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Casida, J. E. and Quistad, G. B. (eds.) (1995) Pyrethrum Flowers: Production, Chemistry, Toxicology, and Uses. Oxford University Press, NY, p. 356.

    Google Scholar 

  2. Elliott, M. (1995) Chemicals in insect control, in Pyrethrum Flowers: Production, Chemistry, Toxicology, and Uses (Casida, J. E. and Quistad, G. B., eds.), Oxford University Press, NY, pp. 3–31.

    Google Scholar 

  3. Casida, J. E. and Quistad, G. B. (1998) Golden age of insecticide research: past, present, or future’? Ann. Rev. Entomol. 43, 1–16.

    Article  CAS  Google Scholar 

  4. Gray, A. J. and Soderlund, D. M. (1985) Mammalian toxicology of pyrethroids, in Insecticides ( Hutson, D. H. and Roberts, T. R., eds.), Wiley, NY, pp. 193–248.

    Google Scholar 

  5. Elliott, M., Farnham, A. W., Janes, N. F., Needham, P. H., and Pulman, D. A. (1974) Insecticidally active conformations of pyrethroids, in Mechanism of Pesticide Action ( Kohn, G. K., ed.), American Chemical Society, Washington, DC, pp. 80–91.

    Chapter  Google Scholar 

  6. Verschoyle, R. D. and Aldridge, W. N. (1980) Structure-activity relationships of some pyrethroids in rats. Arch. Toxicol. 45, 325–329.

    Article  PubMed  CAS  Google Scholar 

  7. Lawrence, L. J. and Casida, J. E. (1982) Pyrethroid toxicology: mouse intracerebral structure-toxicity relationships. Pestic. Biochem. Physiol. 18, 9–14.

    Article  CAS  Google Scholar 

  8. Ghiasuddin, S. M. and Soderlund, D. M. (1985) Pyrethroid insecticides: potent, stereospecific enhancers of mouse brain sodium channel activation. Pestic. Biochem. Physiol. 24, 200–206.

    Article  CAS  Google Scholar 

  9. Verschoyle, R. D. and Barnes, J. M. (1972) Toxicity of natural and synthetic pyrethrins to rats. Pestic. Biochem. Physiol. 2, 308–311.

    Article  CAS  Google Scholar 

  10. Elliott, M., Farnham, A. W., Janes, N. F., Needham, P. H., and Pulman, D. A. (1974) Synthetic insecticide with a new order of activity. Nature 248, 710–711.

    Article  PubMed  CAS  Google Scholar 

  11. Barnes, J. M. and Verschoyle, R. D. (1974) Toxicity of new pyrethroid insecticide. Nature 248, 711.

    Article  PubMed  CAS  Google Scholar 

  12. Gammon, D. W., Brown, M. A., and Casida, J. E. (1981) Two classes of pyrethroid action in the cockroach. Pestic. Biochem. Physiol. 15, 181–191.

    Article  CAS  Google Scholar 

  13. He, F., Wang, S., Liu, L., Chen, S., Zhang, Z., and Sun, J. (1989) Clinical manifestations and diagnosis of acute pyrethroid poisoning. Arch. Toxicol. 63, 54–58.

    Article  PubMed  CAS  Google Scholar 

  14. Lessenger, J. E. (1992) Five office workers inadvertently exposed to cypermethrin. J. Toxicol. Environ. Health 35, 261–267.

    Article  PubMed  CAS  Google Scholar 

  15. Box, S. A. and Lee, M. R. (1996) A systemic reaction following exposure to a pyrethroid insecticide. Hum. Exp. Toxicol. 15, 389–390.

    Article  PubMed  CAS  Google Scholar 

  16. Gotoh, Y., Kawakami, M., Matsumoto, N., and Okada, Y. (1998) Permethrin emulsion ingestion: clinical manifestations and clearance of isomers. Clin. Toxicol. 36, 57–61.

    Article  CAS  Google Scholar 

  17. Vijverberg, H. P. M. and van den Bercken, J. (1990) Neurotoxicological effects and the mode of action of pyrethroid insecticides. CRC Crit. Rev. Toxicol. 21, 105–126.

    Article  CAS  Google Scholar 

  18. Clark, J. M. (1995) Effects and mechanisms of action of pyrethrin and pyrethroid insecticides, in Handbook of Neurotoxicology ( Chang, L. W. and Dyer, R. S., eds.), Marcel Dekker, NY, pp. 511–546.

    Google Scholar 

  19. Flannigan, S. A. and Tucker, S. B. (1985) Variation in cutaneous sensation between synthetic pyrethroid insecticides. Contact Dermatitis 13, 140–147.

    Article  PubMed  CAS  Google Scholar 

  20. Cagen, S. Z., Malley, L. A., Parker, C. M., Gardiner, T. H., van Gelder, G. A., and Jud, V. A. (1984) Pyrethroid-mediated skin sensory stimulation characterized by a new behavioral paradigm. Toxicol. Appl. Pharmacol. 76, 270–279.

    Article  PubMed  CAS  Google Scholar 

  21. Rizzo, M. A., Kocsis, J. D., and Waxman, S. G. (1996) Mechanisms of paresthesiae, dysthesiae, and hyperesthesia: role of Na+ channel heterogeneity. Eur. Neurol. 36, 1–12.

    Article  Google Scholar 

  22. Soderlund, D. M. and Bloomquist, J. R. (1989) Neurotoxic actions of pyrethroid insecticides. Ann. Rev. Entomol. 34, 77–96.

    Article  CAS  Google Scholar 

  23. Narahashi, T. (1992) Nerve membrane Na+ channels as targets of insecticides. Trends Pharmacol. Sci. 13, 236–241.

    Article  PubMed  CAS  Google Scholar 

  24. Bloomquist, J. R. (1993) Neuroreceptor mechanisms in pyrethroid mode of action and resistance, in Reviews in Pesticide Toxicology ( Roe, M. and Kuhr, R. J., eds.), Toxicology Communications, Raleigh, NC, pp. 181–226.

    Google Scholar 

  25. Soderlund, D. M. (1995) Mode of action of pyrethrins and pyrethroids, in Pyrethrum Flowers: Production, Chemistry, Toxicology, and Uses (Casida, J. E. and Quistad, G. B., eds.), Oxford University Press, NY, pp. 217–233.

    Google Scholar 

  26. Bloomquist, J. R. (1996) Ion channels as targets for insecticides. Ann. Rev. Entomol. 41, 163–190.

    Article  CAS  Google Scholar 

  27. Narahashi, T. (1996) Neuronal ion channels as the target sites of insecticides. Pharmacol. Toxicol. 78, 1–14.

    Article  Google Scholar 

  28. Lund, A. E. and Narahashi, T. (1983) Kinetics of sodium channel modification as the basis for the variation in the nerve membrane effects of pyrethroids and DDT analogs. Pestic. Biochem. Physiol. 20, 203–216.

    Article  CAS  Google Scholar 

  29. Vijverberg, H. P. M., van der Zalm, J. M., van Kleef, R. G. D. M., and van den Bercken, J. (1983) Temperature-and structure-dependent interaction of pyrethroids with the sodium channels in frog node of Ranvier. Biochim. Biophys. Acta 728, 73–82.

    Article  PubMed  CAS  Google Scholar 

  30. Yamamoto, D., Quandt, F. N., and Narahashi, T. (1983) Modification of single sodium channels by tetramethrin. Brain Res. 274, 344–349.

    Article  PubMed  CAS  Google Scholar 

  31. Chinn, K. and Narahashi, T. (1986) Stabilization of sodium channel states by deltamethrin in mouse neuroblastoma cells. J. Physiol. 380, 191–207.

    PubMed  CAS  Google Scholar 

  32. Holloway, S. F., Salgado, V. L., Wu, C. H., and Narahashi, T. (1989) Kinetic properties of single sodium channels modified by fenvalerate in mouse neuroblastoma cells. Pflugers Arch. 414, 613–621.

    Article  PubMed  CAS  Google Scholar 

  33. Soderlund, D. M., Bloomquist, J. R., Ghiasuddin, S. M., and Stuart, A. M. (1987) Enhancement of veratridine-dependent sodium channel activation by pyrethroids and DDT analogs, in Sites of Action for Neurotoxic Pesticides ( Hollingworth, R. M. and Green, M. B., eds.), American Chemical Society, Washington, DC, pp. 251–261.

    Chapter  Google Scholar 

  34. Bloomquist, J. R. and Soderlund, D. M. (1988) Pyrethroid insecticides and DDT modify alkaloid-dependent sodium channel activation and its enhancement by sea anemone toxin. Mol. Pharmacol. 33, 543–550.

    PubMed  CAS  Google Scholar 

  35. Brown, G. B., Gaupp, J. E. and Olsen, R. W. (1988) Pyrethroid insecticides: stereospecific allosteric interaction with the batrachotoxinin-A benzoate binding site of mammalian voltage-sensitive sodium channels. Mol. Pharmacol. 34, 54–59.

    PubMed  CAS  Google Scholar 

  36. Lombet, A., Mourre, C., and Lazdunski, M. (1988) Interactions of insecticides of the pyrethroid family with specific binding sites on the voltage-dependent sodium channel from mammalian brain. Brain Res. 459, 44–53.

    Article  PubMed  CAS  Google Scholar 

  37. Rubin, J. G., Payne, G. T., and Soderlund, D. M. (1993) Structure-activity relationships for pyrethroids and DDT analogs as modifiers of [3H]batrachotoxinin A 20-a-benzoate binding to mouse brain sodium channels. Pestic. Biochem. Physiol. 45, 130–140.

    Article  CAS  Google Scholar 

  38. Soderlund, D. M., Ghiasuddin, S. M., and Helmuth, D. W. (1983) Receptor-like stereospecific binding of a pyrethroid insecticide to mouse brain membranes. Life Sci. 33, 261–267.

    Article  PubMed  CAS  Google Scholar 

  39. Trainer, V. L., McPhee, J. C., Boutelet-Bochan, H., Baker, C., Scheuer, T., Babin, D., et al. (1997) High affinity binding of pyrethroids to the a subunit of brain sodium channels. Mol. Pharmacol. 51, 651–657.

    PubMed  CAS  Google Scholar 

  40. Forshaw, P. J. and Bradbury, J. E. (1983) Pharmacological effects of pyrethroids on the cardiovascular system of the rat. Eur. J. Pharmacol. 91, 207–213.

    Article  PubMed  CAS  Google Scholar 

  41. Berlin, J. R., Akera, T., Brody, T. M., and Matsumura, F. (1984) The inotropic effects of a synthetic pyrethroid decamethrin on isolated guinea pig atrial muscle. Eur. J. Pharmacol. 98, 313–322.

    Article  PubMed  CAS  Google Scholar 

  42. Daly, J. W., McNeal, E. T., and Gusovsky, F. (1987) Cardiotonic activities of pumiliotoxin B, pyrethroids and a phorbol ester and their relationships with phosphoinositide turnover. Biochim. Biophys. Acta 930, 470–474.

    Article  PubMed  CAS  Google Scholar 

  43. Forshaw, P. J. and Ray, D. E. (1986) The effects of two pyrethroids, cismethrin and deltamethrin, on skeletal muscle and the trigeminal reflex system in the rat. Pestic. Biochem. Physiol. 25, 143–151.

    Article  CAS  Google Scholar 

  44. Forshaw, P. J., Lister, T., and Ray, D. E. (1987) The effects of two types of pyrethroid on rat skeletal muscle. Eur. J. Pharmacol. 134, 89–96.

    Article  PubMed  CAS  Google Scholar 

  45. Wright, C. D. P., Forshaw, P. J., and Ray, D. E. (1988) Classification of the actions of ten pyrethroid insecticides in the rat, using the trigeminal reflex and skeletal muscle as test systems. Pestic. Biochem. Physiol. 30, 79–86.

    Article  CAS  Google Scholar 

  46. Ginsburg, K. S. and Narahashi, T. (1993) Differential sensitivity of tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels to the insecticide allethrin in rat dorsal root ganglion neurons. Brain Res. 627, 239–248.

    Article  PubMed  CAS  Google Scholar 

  47. Tatebayashi, H. and Narahashi, T. (1994) Differential mechanism of action of the pyrethroid tetramethrin on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels. J. Pharmacol. Exp. Ther. 270, 595–603.

    PubMed  CAS  Google Scholar 

  48. Song, J.-H. and Narahashi, T. (1996) Differential effects of the pyrethroid tetramethrin on tetrodotoxin-sensitive and tetrodotoxin-resistant single sodium channels. Brain Res. 712, 258–264.

    Article  PubMed  CAS  Google Scholar 

  49. Tabarean, I. V. and Narahashi, T. (1998) Potent modulation of tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels by the Type I1 pyrethroid deltamethrin. J. Pharmacol. Exp. Ther. 284, 958–965.

    PubMed  CAS  Google Scholar 

  50. Lester, H. A. (1988) Heterologous expression of excitability proteins: route to more specific drugs? Science 241, 1057–1063.

    Article  PubMed  CAS  Google Scholar 

  51. Auld, V. J., Goldin, A. L., Krafte, D. S., Marshall, J., Dunn, J. M., Catterall, W. A., et al. (1988) A rat brain Na+ channel a subunit with novel gating properties. Neuron 1, 449–461.

    Article  PubMed  CAS  Google Scholar 

  52. Smith, T. J. and Soderlund, D. M. (1998) Action of the pyrethroid insecticide cypermethrin on rat brain IIa sodium channels expressed in Xenopus oocytes. NeuroToxicology 19, 823–832.

    CAS  Google Scholar 

  53. Smith, T. J. and Soderlund, D. M. (2000) Structure-activity relationships for the action of deltamethrin analogs on sodium channels expressed in Xenopus oocytes. Soc. Neurosci. Abst. 22, 60.

    Google Scholar 

  54. Akopian, A. N., Sivilotti, L., and Wood, J. N. (1996) A tetrodotoxin-resistant voltage-gated sodium channel expressed in sensory neurons. Nature 379, 257–262.

    Article  PubMed  CAS  Google Scholar 

  55. Sangameswaran, L., Delagado, S. G., Fish, L. M., Koch, B. D., Jakeman, L. B., Stewart, G. R., et al. (1996) Structure and function of a novel voltage-gated, tetrodotoxin-resistant sodium channel specific to sensory neurons. J. Biol. Chem. 271, 5953–5956.

    Article  PubMed  CAS  Google Scholar 

  56. Smith, T. J. and Soderlund, D. M. (2000) Potent actions of the pyrethroid insecticides cismethrin and cypermethrin on rat tetrodotoxin-resistant peripheral nerve (SNS/PN3) sodium channels expressed in Xenopus oocytes. Pestic. Biochem. Physiol. 70, 52–61.

    Article  Google Scholar 

  57. Leeb-Lundberg, F. and Olsen, R. W. (1980) Picrotoxinin binding as a probe of the GABA postsynaptic membrane receptor-ionophore complex, in Psychopharmacology and Biochemistry of Neurotransmitter Receptors ( Yamamura, H. I., Olsen, R. W., and Usdin, E., eds.), Elsevier, NY, pp. 593–606.

    Google Scholar 

  58. Lawrence, L. J. and Casida, J. E. (1983) Stereospecific action of pyrethroid insecticides on the y-aminobutyric acid receptor-ionophore complex. Science 221, 1399–1401.

    Article  PubMed  CAS  Google Scholar 

  59. Casida, J. E. and Lawrence, L. J. (1985) Structure-activity correlations for interactions of bicyclophosphorus esters and some polychlorocycloalkane and pyrethroid insecticides with the brain-specific t-butylbicyclophosphorothionate receptor. Environ. Health Perspec. 61, 123–132.

    Article  CAS  Google Scholar 

  60. Bloomquist, J. R. and Soderlund, D. M. (1985) Neurotoxic insecticides inhibit GABAdependent chloride uptake by mouse brain vesicles. Biochem. Biophys. Res. Commun. 133, 37–43.

    Article  PubMed  CAS  Google Scholar 

  61. Bloomquist, J. R., Adams, P. M., and Soderlund, D. M. (1986) Inhibition ofy-aminobutyric acid-stimulated chloride flux in mouse brain vesicles by polychlorocycloalkane and pyrethroid insecticides. NeuroToxicology 7, 11–20.

    PubMed  CAS  Google Scholar 

  62. Abalis, I. M., Eldefrawi, M. E., and Eldefrawi, A. T. (1986) Effects of insecticides on GABA-induced chloride influx into rat brain microsacs. J. Toxicol. Environ. Health 18, 13–23.

    Article  PubMed  CAS  Google Scholar 

  63. Ramadan, A. A., Bakry, N. M., Marei, A. S. M., Eldefrawi, A. T., and Eldefrawi, M. E. (1988) Action of pyrethroids on GABAA receptor function. Pestic. Biochem. Physiol. 32, 97–105.

    Article  CAS  Google Scholar 

  64. Ogata, N., Vogel, S. M., and Narahashi, T. (1988) Lindane but not deltamethrin blocks a component of GABA-activated chloride channels. FASEB J. 2, 2895–2900.

    PubMed  CAS  Google Scholar 

  65. Gilbert, M. E., Mack, C. M., and Crofton, K. M. (1989) Pyrethroids and enhanced inhibition in the hippocampus of the rat. Brain Res. 477, 314–321.

    Article  PubMed  CAS  Google Scholar 

  66. Joy, R. M., Albertson, T. E., and Ray, D. E. (1989) Type I and Type II pyrethroids increase inhibition in the hippocampal dentate gyrus of the rat. Toxicol. Appl. Pharmacol. 98, 398–412.

    Article  PubMed  CAS  Google Scholar 

  67. Joy, R. M., Lister, T., Ray, D. E., and Seville, M. P. (1990) Characteristics of the prolonged inhibition produced by a range of pyrethroids in the rat hippocampus. Toxicol. Appl. Pharmacol. 103, 528–538.

    Article  PubMed  CAS  Google Scholar 

  68. Joy, R. M. and Albertson, T. E. (1991) Interactions of GABAA antagonists with deltamethrin, diazepam, pentobarbital, and SKF100330A in the rat dentate gyms. Toxicol. Appl. Pharmacol. 109, 251–262.

    Article  PubMed  CAS  Google Scholar 

  69. Forshaw, P. J. and Ray, D. E. (1990) A novel action of deltamethrin on membrane resistance in mammalian skeletal muscle and non-myelinated nerve fibers. Neuropharmacology 29, 75–81.

    Article  CAS  Google Scholar 

  70. Abalis, I. M., Eldefrawi, A. T., and Eldefrawi, M. E. (1986) Actions of avermectin Bla on the y-aminobutyric acidA receptor and chloride channels in rat brain. J. Biochem. Toxicol. 1, 69–82.

    Article  PubMed  CAS  Google Scholar 

  71. Forshaw, P. J., Lister, T., and Ray, D. E. (1993) Inhibition of a neuronal voltage-dependent chloride channel by the Type II pyrethroid deltamethrin. Neuropharmacology 32, 105–111.

    Article  PubMed  CAS  Google Scholar 

  72. Ray, D. E., Sutharsan, S., and Forshaw, P. J. (1997) Action of pyrethroid insecticides on voltage-gated chloride channels in neuroblastoma cells. NeuroToxicology 18, 755–760.

    PubMed  CAS  Google Scholar 

  73. Ray, D. E., Lister, T., and Forshaw, P. J. (1999) A new basis for therapy against Type-II pyrethroid poisoning, in Progress in Neuropharmacology and Neurotoxicology of Pesticides and Drugs ( Beadle, D. J., ed.), Royal Society of Chemistry, Cambridge, UK, pp. 204–214.

    Google Scholar 

  74. Forshaw, P. J., Lister, T., and Ray, D. E. (2000) The role of voltage-gated chloride channels in type II pyrethroid insecticide poisoning. Toxicol. Appl. Pharmacol. 163, 1–8.

    Article  PubMed  CAS  Google Scholar 

Download references

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 2002 Springer Science+Business Media New York

About this chapter

Cite this chapter

Soderlund, D.M. (2002). Agents Affecting Sodium Channels. In: Massaro, E.J. (eds) Handbook of Neurotoxicology. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-59259-132-9_4

Download citation

  • DOI: https://doi.org/10.1007/978-1-59259-132-9_4

  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-61737-193-6

  • Online ISBN: 978-1-59259-132-9

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics