Protein Information

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

Compound Information

Name cypermethrin
CAS cyano(3-phenoxyphenyl)methyl 3-(2,2-dichloroethenyl)-2,2-dimethylcyclopropanecarboxylate

Reference List

PubMed Abstract RScore(About this table)
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.

Four of six alpha-cyano pyrethroids (lambda-cyfluthrin, cypermethrin, deltamethrin and fenpropathrin) reduced open chloride channel probability.
82(1,1,1,2) Details
17603033 Borg JJ, Hancox JC, Zhang H, Spencer CI, Li H, Kozlowski RZ: Differential pharmacology of the cardiac anionic background current I (AB). Eur J Pharmacol. 2007 Aug 27;569(3):163-70. Epub 2007 Jun 5.

This study investigated the effects of on I (AB) of four pyrethroid agents tefluthrin (a selective activator of this current), tetramethrin, fenpropathrin and alpha-cypermethrin in addition to other well known chloride channel modulators (chlorotoxin, gadolinium and picrotoxin).
31(0,1,1,1) Details
8054658 Bloomquist JR: Cyclodiene resistance at the insect GABA receptor/chloride channel complex confers broad cross resistance to convulsants and experimental phenylpyrazole insecticides. Arch Insect Biochem Physiol. 1994;26(1):69-79.

In contrast, this strain was susceptible to cypermethrin and the avermectins MK-243, abamectin, and abamectin 8,9-oxide.
3(0,0,0,3) Details
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.
2(0,0,0,2) Details
1787887 Eshleman AJ, Murray TF: Pyrethroid insecticides indirectly inhibit GABA-dependent 36Cl- influx in synaptoneurosomes from the trout brain. Neuropharmacology. 1991 Dec;30(12A):1333-41.

Deltamethrin, (1R alpha S)-cis-cypermethrin and permethrin produced a dose-dependent increase in the basal uptake and a corresponding decrease in GABA-dependent influx, with a maximum inhibition of 70-82%.
Thus, pyrethroid insecticides may interfere with the function of GABAA receptors indirectly through an interaction with the voltage-dependent sodium channel in the brain of the trout and consequently perturb chloride influx, possibly through a voltage-dependent chloride channel.
1(0,0,0,1) Details
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.
1(0,0,0,1) Details