Protein Information

Name chloride channel (protein family or complex)
Synonyms chloride channel

Compound Information

Name cismethrin
CAS

Reference List

PubMed Abstract RScore(About this table)
10662599 Forshaw PJ, Lister T, Ray DE: The role of voltage-gated chloride channels in type II pyrethroid insecticide poisoning. Toxicol Appl Pharmacol. 2000 Feb 15;163(1):1-8.

In the present study we evaluated potential chloride channel agonists in vitro, and then tested the most effective of these on pyrethroid-poisoned rats to determine the practical significance of chloride channel effects in vivo.
This was followed by deltamethrin (1.5 or 2 mg/kg iv) or the type I pyrethroid cismethrin (4 mg/kg iv).
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19766671 Breckenridge CB, Holden L, Sturgess N, Weiner M, Sheets L, Sargent D, Soderlund DM, Choi JS, Symington S, Clark JM, Burr S, Ray D: Evidence for a separate mechanism of toxicity for the Type I and the Type II pyrethroid insecticides. Neurotoxicology. 2009 Nov;30 Suppl 1:S17-31. Epub 2009 Sep 18.

Neurotoxicity and mechanistic data were collected for six alpha-cyano pyrethroids (beta-cyfluthrin, cypermethrin, deltamethrin, esfenvalerate, fenpropathrin and lambda-cyhalothrin) and up to six non-cyano containing pyrethroids (bifenthrin, S-bioallethrin [or allethrin], permethrin, pyrethrins, resmethrin [or its cis-isomer, cismethrin] and tefluthrin under standard conditions.
Factor analysis and multivariate dissimilarity analysis were employed to evaluate four independent data sets comprised of (1) fifty-six behavioral and physiological parameters from an acute neurotoxicity functional observatory battery (FOB), (2) eight electrophysiological parameters from voltage clamp experiments conducted on the Na (v) 1.8 sodium channel expressed in Xenopus oocytes, (3) indices of efficacy, potency and binding calculated for calcium ion influx across neuronal membranes, membrane depolarization and glutamate released from rat brain synaptosomes and (4) changes in chloride channel open state probability using a patch voltage clamp technique for membranes isolated from mouse neuroblastoma cells.
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9339822 Ray DE, Sutharsan S, Forshaw PJ: Actions of pyrethroid insecticides on voltage-gated chloride channels in neuroblastoma cells. Neurotoxicology. 1997;18(3):755-60.

We have assessed one such site, the voltage gated chloride channel.
A second Type II pyrethroid cypermethrin also decreased P0, by 0.430+/-0.09 at 5 x 10 (-6) M, but the Type I pyrethroid cismethrin produced a decrease of only 0.188+/-0.08 at 2 x 10 (-5) M.
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14657519 Burr SA, Ray DE: Structure-activity and interaction effects of 14 different pyrethroids on voltage-gated chloride ion channels. Toxicol Sci. 2004 Feb;77(2):341-6. Epub 2003 Dec 2.

It therefore appears clear that in some combinations the type I and type II pyrethroids can compete and may bind to the same chloride channel target site.
We have proposed that since the type II pyrethroids deltamethrin and cypermethrin, but not the type I pyrethroid cismethrin act on chloride channels, this could contribute to the bimodal nature of pyrethroid poisoning syndromes.
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