| Name | sodium channel (protein family or complex) |
|---|---|
| Synonyms | Sodium channel |
| Name | permethrin |
|---|---|
| CAS | (3-phenoxyphenyl)methyl 3-(2,2-dichloroethenyl)-2,2-dimethylcyclopropanecarboxylate |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 11095943 | Zhao Y, Park Y, Adams ME: Functional and evolutionary consequences of pyrethroid resistance mutations in S6 transmembrane segments of a voltage-gated sodium channel. Biochem Biophys Res Commun. 2000 Nov 30;278(3):516-21. We analyzed the consequences of V421M and L1029H mutations constructed in the Drosophila para sodium channel heterologously expressed in Xenopus oocytes, and found that both mutations confer channel insensitivity to permethrin, with the L1029H mutation having a more pronounced effect. |
9(0,0,1,4) | Details |
| 15271210 | Ranson H, Paton MG, Jensen B, McCarroll L, Vaughan A, Hogan JR, Hemingway J, Collins FH: Genetic mapping of genes conferring permethrin resistance in the malaria vector, Anopheles gambiae. Insect Mol Biol. 2004 Aug;13(4):379-86. The first QTL, rtp1, colocalizes with the sodium channel gene on chromosome 2L thus further supporting the importance of mutations in this gene in conferring permethrin resistance. |
7(0,0,1,2) | Details |
| 16051293 | Choi JS, Soderlund DM: Structure-activity relationships for the action of 11 pyrethroid insecticides on rat Na v 1.8 channels expressed in Xenopus oocytes. Toxicol Appl Pharmacol. 2006 Mar 15;211(3):233-44. Epub 2005 Jul 26. This paper describes the action of 11 structurally diverse commercial pyrethroid insecticides on the rat Na v 1.8 sodium channel isoform, the principal carrier of the tetrodotoxin-resistant, pyrethroid-sensitive current of sensory neurons, expressed in Xenopus laevis oocytes. All 11 compounds produced characteristic tail currents following a depolarizing pulse that ranged from rapidly-decaying monoexponential currents (allethrin, cismethrin and permethrin) to persistent biexponential currents (cyfluthrin, cyhalothrin, cypermethrin and deltamethrin). |
1(0,0,0,1) | Details |
| 2546657 | Gusovsky F, Secunda SI, Daly JW: Pyrethroids: involvement of channels in effects on formation in guinea pig synaptoneurosomes. Brain Res. 1989 Jul 17;492(1-2):72-8. Type II pyrethroids, like deltamethrin and fenvalerate, were more potent and, at least for deltamethrin, more efficacious than type I pyrethroids, like allethrin, resmethrin and permethrin. The effects of type II pyrethroids could be partially inhibited by the sodium channel blocker tetrodotoxin. |
1(0,0,0,1) | Details |
| 9443375 | Guerrero FD, Jamroz RC, Kammlah D, Kunz SE: Toxicological and molecular characterization of pyrethroid-resistant horn flies, Haematobia irritans: identification of kdr and super-kdr point mutations. Insect Biochem Mol Biol. 1997 Aug-Sep;27(8-9):745-55. Two pyrethroid-resistant strains of horn flies were found to be 17- and 688-fold more resistant to permethrin and 17- and 11,300-fold more resistant to cyhalothrin than a susceptible control strain. Using the reverse transcriptase-polymerase chain reaction (RT-PCR), a 0.9 kb fragment of the putative sodium channel gene from susceptible and resistant flies was cloned and sequenced. |
1(0,0,0,1) | Details |
| 16363167 | Kristensen M: Identification of sodium channel mutations in human head louse (Anoplura: Pediculidae) from Denmark. J Med Entomol. 2005 Sep;42(5):826-9. The presence of the two mutations T9291-L932F in the voltage-sensitive sodium channel gene associated with permethrin resistance (kdr-like) was shown in head louse, Pediculus humanus capitis De Geer, populations in Denmark. |
7(0,0,1,2) | Details |
| 18533436 | Li AY, Davey RB, Miller RJ, Guerrero FD, George JE: Genetics and mechanisms of permethrin resistance in the Santa Luiza strain of Boophilus microplus (Acari: Ixodidae). J Med Entomol. 2008 May;45(3):427-38. The results of this study suggest that other mechanisms, including a possible new sodium channel mutation that is different from the one currently known, may be responsible for permethrin resistance in the Santa Luiza strain of B. microplus. |
6(0,0,1,1) | Details |
| 16221961 | Wolansky MJ, Gennings C, Crofton KM: Relative potencies for acute effects of pyrethroids on motor function in rats. Toxicol Sci. 2006 Jan;89(1):271-7. Epub 2005 Oct 12. A common mode-of-action has been proposed for pyrethroids based on in vitro studies, which includes alterations in sodium channel dynamics in nervous system tissues, consequent disturbance of membrane polarization, and abnormal discharge in targeted neurons. Acute oral dose-response functions were determined in adult male Long Evans rats for five Type I (bifenthrin, S-bioallethrin, permethrin, resmethrin, tefluthrin), five Type II (beta-cyfluthrin, lambda-cyhalothrin, cypermethrin, deltamethrin, esfenvalerate) and one mixed Type I/II (fenpropathrin) pyrethroids (n = 8-18 per dose; 6-11 dose levels per chemical, vehicle = corn oil, at 1 ml/kg). |
1(0,0,0,1) | Details |
| 17427702 | Miller RJ, Davey RB, George JE: First report of permethrin-resistant Boophilus microplus (Acari: Ixodidae) collected within the United States. J Med Entomol. 2007 Mar;44(2):308-15. Polymerase chain reaction examination revealed the presence of a mutation of the sodium channel gene [arrow] amino acid substitution in the S6 trans-membrane segment of domain III), in the resistant B&H; population. |
1(0,0,0,1) | Details |
| 6276777 | Vijverberg HP, van der Zalm JM, van der Bercken J: Similar mode of action of pyrethroids and DDT on sodium channel gating in myelinated nerves. Nature. 1982 Feb 18;295(5850):601-3. |
1(0,0,0,1) | Details |
| 19829709 | Garcia GP, Flores AE, Fernandez-Salas I, Saavedra-Rodriguez K, Reyes-Solis G, Lozano-Fuentes S, Guillermo Bond J, Casas-Martinez M, Ramsey JM, Garcia-Rejon J, Dominguez-Galera M, Ranson H, Hemingway J, Eisen L, Black IV WC: Recent rapid rise of a permethrin knock down resistance allele in Aedes aegypti in Mexico. PLoS Negl Trop Dis. 2009 Oct 13;3(10):e531. In 2007, we documented a replacement mutation in codon 1,016 of the voltage-gated sodium channel gene (para) of Ae. aegypti that encodes an rather than a and confers resistance to permethrin. |
7(0,0,1,2) | Details |
| 18826035 | Kwon DH, Yoon KS, Strycharz JP, Clark JM, Lee SH: Determination of permethrin resistance allele frequency of human head louse populations by quantitative sequencing. J Med Entomol. 2008 Sep;45(5):912-20. A quantitative sequencing (QS) protocol that detects the frequencies of sodium channel mutations (M815I, T917I, and L920F) responsible for knockdown resistance in permethrin-resistant head lice (Pediculus humanus capitis De Geer) was tested as a population genotyping method for use as a preliminary resistance monitoring tool. |
7(0,0,1,2) | Details |
| 18051777 | Djadid ND, Forouzesh F, Karimi M, Raeisi A, Hassan-Zehi A, Zakeri S: Monitoring pyrethroid insecticide resistance in major malaria vector Anopheles culicifacies: comparison of molecular tools and conventional susceptibility test. Iran Biomed J. 2007 Jul;11(3):169-76. METHODS: In current study, along with WHO routine susceptibility test with DDT (4%), dieldrin (0.4%), malathion (5%), permethrin (0.25%), lambadacyhalothrin (0.1%), and deltamethrin 0.025, we cloned and sequenced segment VI of domain II (SII6) in voltage-gated sodium channel (vgsc) gene of An. culicifacies specimens collected in Sistan and Baluchistan province (Iran). |
6(0,0,1,1) | Details |
| 12823830 | Enayati AA, Vatandoost H, Ladonni H, Townson H, Hemingway J: Molecular evidence for a kdr-like pyrethroid resistance mechanism in the malaria vector mosquito Anopheles stephensi. Med Vet Entomol. 2003 Jun;17(2):138-44. Activities of some enzymes likely to confer pyrethroid-resistance (i.e. esterases, monooxygenases and glutathione S-transferases) were significantly higher in the permethrin-resistant than in the susceptible strain, but the use of synergists--piperonyl butoxide (PBO) to inhibit monooxygenases and/or tribufos (DEF) to inhibit esterases--did not fully prevent resistance in larvae (permethrin LC50 reduced by only 51-68%), indicating the involvement of another mechanism. From both strains of An. stephensi, we obtained a 237-bp fragment of genomic DNA encoding segment 6 of domain II of the para type voltage-gated sodium channel, i.e. the putative kdr locus. |
1(0,0,0,1) | Details |
| 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 influx across neuronal membranes, membrane depolarization and 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. |
1(0,0,0,1) | Details |
| 17896620 | Awolola TS, Oduola AO, Oyewole IO, Obansa JB, Amajoh CN, Koekemoer LL, Coetzee M: Dynamics of knockdown pyrethroid insecticide resistance alleles in a field population of Anopheles gambiae s.s. in southwestern Nigeria. J Vector Borne Dis. 2007 Sep;44(3):181-8. Insecticide susceptibility tests did not show any significant increase in the resistance status recorded for either Permethrin or DDT from 2002-05, rather, an improvement in the susceptibility status of the mosquitoes to these insecticides was observed from 2004-05 relative to the tests performed in 2002-03. BACKGROUND & OBJECTIVES: Pyrethroid insecticide resistance in the malaria vector Anopheles gambiae Giles is mainly associated with reduced target site sensitivity arising from a single point mutation in the sodium channel gene, often referred to as knockdown resistance (kdr). |
1(0,0,0,1) | Details |
| 18723882 | Saavedra-Rodriguez K, Strode C, Flores Suarez A, Fernandez Salas I, Ranson H, Hemingway J, Black WC 4th: Quantitative trait loci mapping of genome regions controlling permethrin resistance in the mosquito Aedes aegypti. Genetics. 2008 Oct;180(2):1137-52. Epub 2008 Aug 24. One corresponds with a SNP previously associated with permethrin resistance in the para sodium channel gene and the second with the CCEunk7o esterase marker. |
6(0,0,1,1) | Details |
| 17915510 | Durand R, Millard B, Bouges-Michel C, Bruel C, Bouvresse S, Izri A: Detection of pyrethroid resistance gene in head lice in schoolchildren from Bobigny, France. J Med Entomol. 2007 Sep;44(5):796-8. Recent studies showed that a M815I-T929I-L932F kdr-like mutation in the voltage-gated sodium channel alpha-subunit gene was associated with permethrin resistance in head lice from several countries worldwide. |
6(0,0,1,1) | Details |
| 15119600 | Corbel V, Raymond M, Chandre F, Darriet F, Hougard JM: Efficacy of insecticide mixtures against larvae of Culex quinquefasciatus (Say) (Diptera: Culicidae) resistant to pyrethroids and carbamates. Pest Manag Sci. 2004 Apr;60(4):375-80. The efficacy of insecticide mixtures of permethrin (pyrethroid) and propoxur was tested by larval bioassays on two strains of Culex quinquefasciatus (Say), one resistant to pyrethroids and the other resistant to carbamates. Nevertheless, antagonism in the R-LAB strain is probably due to a physiological perturbation implying different target sites for pyrethroid (ie sodium channel) and insecticides [ie acetylcholinesterase (EC 3.3.3.7) and choline acetyltransferase (EC 2.3.1.6)]. |
1(0,0,0,1) | Details |
| 16678264 | Meyer DA, Shafer TJ: Permethrin, but not deltamethrin, increases spontaneous release from hippocampal neurons in culture. Neurotoxicology. 2006 Jul;27(4):594-603. Epub 2006 Mar 28. Pyrethroid insecticide modulation of the voltage-gated sodium channel (VGSC) is proposed to underlie their effects on neuronal excitability. |
1(0,0,0,1) | Details |
| 18402142 | Reimer L, Fondjo E, Patchoke S, Diallo B, Lee Y, Ng A, Ndjemai HM, Atangana J, Traore SF, Lanzaro G, Cornel AJ: Relationship between kdr mutation and resistance to pyrethroid and DDT insecticides in natural populations of Anopheles gambiae. J Med Entomol. 2008 Mar;45(2):260-6. Two mutations at the same locus in the voltage-gated sodium channel gene are known to confer knockdown resistance (kdr) to pyrethroids and DDT. Kdr-w conferred greater resistance to permethrin than kdr-e. |
1(0,0,0,1) | Details |
| 14651650 | McMahon C, Krober T, Guerin PM: In vitro assays for repellents and deterrents for ticks: differing effects of products when tested with attractant or arrestment stimuli. Med Vet Entomol. 2003 Dec;17(4):370-8. The effect of permethrin, a sodium channel blocker, was also tested in a deterrent assay measuring the arrestment of Ixodes ricinus (L.) adults on its own faeces and faecal constituents. |
6(0,0,1,1) | Details |
| 17089332 | Yu SJ, McCord E Jr: Lack of cross-resistance to indoxacarb in insecticide-resistant Spodoptera frugiperda (Lepidoptera: Noctuidae) and Plutella xylostella (Lepidoptera: Yponomeutidae). Pest Manag Sci. 2007 Jan;63(1):63-7. The lack of cross-resistance between indoxacarb and permethrin in P. xylostella further supports the notion that the mode of action of these insecticides on the insect sodium channel is different. |
6(0,0,1,1) | Details |
| 16607000 | Pasay C, Walton S, Fischer K, Holt D, McCarthy J: PCR-based assay to survey for knockdown resistance to pyrethroid acaricides in human scabies mites (Sarcoptes scabiei var hominis). Am J Trop Med Hyg. 2006 Apr;74(4):649-57. Permethrin, in the form of a topical cream, is being increasingly used for community-based programs to control endemic scabies. The best recognized form of pyrethroid resistance, known as knockdown resistance or kdr, has been linked to specific mutations in the target of these agents, the para-homologous voltage-sensitive sodium channel gene (Vssc). |
1(0,0,0,1) | Details |
| 15210997 | Stump AD, Atieli FK, Vulule JM, Besansky NJ: Dynamics of the pyrethroid knockdown resistance allele in western Kenyan populations of Anopheles gambiae in response to insecticide-treated bed net trials. Am J Trop Med Hyg. 2004 Jun;70(6):591-6. Permethrin and DDT resistance in Anopheles gambiae s.s. associated with a -serine knockdown resistance (kdr) mutation in the voltage-gated sodium channel gene was discovered recently in western Kenya where a large scale permethrin-impregnated bed net (ITN) program has been implemented. |
6(0,0,1,1) | Details |
| 15476966 | Foil LD, Coleman P, Eisler M, Fragoso-Sanchez H, Garcia-Vazquez Z, Guerrero FD, Jonsson NN, Langstaff IG, Li AY, Machila N, Miller RJ, Morton J, Pruett JH, Torr S: Factors that influence the prevalence of acaricide resistance and tick-borne diseases. Vet Parasitol. 2004 Oct 28;125(1-2):163-81. A PCR-based assay to detect a specific sodium channel gene mutation that is associated with resistance to permethrin has been developed. |
6(0,0,1,1) | Details |
| 11695191 | Clark JM, Lee SH, Kim HJ, Yoon KS, Zhang A: DNA-based genotyping techniques for the detection of point mutations associated with insecticide resistance in Colorado potato beetle Leptinotarsa decemlineata. Pest Manag Sci. 2001 Oct;57(10):968-74. Three DNA-based genotyping techniques, bi-directional PCR amplification of specific allele (bi-PASA), single-stranded conformational polymorphism (SSCP) and minisequencing, have been developed and compared for the detection of the S291G (insensitive acetylcholinesterase) and L1014F (insensitive sodium channel) mutations associated with azinphos-methyl and permethrin resistance, respectively, in the Colorado potato beetle (Leptinotarsa decemlineata). |
6(0,0,1,1) | Details |
| 19861644 | DeMicco A, Cooper KR, Richardson JR, White LA: Developmental neurotoxicity of pyrethroid insecticides in zebrafish embryos. Toxicol Sci. 2010 Jan;113(1):177-86. Epub 2009 Oct 27. Treatment with diazepam ameliorated the spasms, while treatment with the sodium channel antagonist MS-222 ameliorated both spasms and body curvature, suggesting that pyrethroid-induced neurotoxicity is similar in zebrafish and mammals. In this study, we sought to investigate the developmental toxicity of six common pyrethroids, three type I compounds (permethrin, resmethrin, and bifenthrin) and three type II compounds (deltamethrin, cypermethrin, and lambda-cyhalothrin), and to determine whether zebrafish embryos may be an appropriate model for studying the developmental neurotoxicity of pyrethroids. |
1(0,0,0,1) | Details |
| 10051544 | Lee D, Park Y, Brown TM, Adams ME: Altered properties of neuronal channels associated with genetic resistance to pyrethroids. Mol Pharmacol. 1999 Mar;55(3):584-93. Pyr-R channels show approximately 21-fold lower sensitivity to the synthetic pyrethroid permethrin and a approximately 2-fold increased sensitivity to the alpha-scorpion toxin LqhalphaIT. |
0(0,0,0,0) | Details |
| 17373952 | Matambo TS, Abdalla H, Brooke BD, Koekemoer LL, Mnzava A, Hunt RH, Coetzee M: Insecticide resistance in the malarial mosquito Anopheles arabiensis and association with the kdr mutation. Med Vet Entomol. 2007 Mar;21(1):97-102. Adults from the F-16 generation of the resistant strain were exposed to all four classes of insecticides approved for use in malaria vector control and showed high levels of resistance to them all (24-h mortalities: malathion, 16.7%; bendiocarb, 33.3%; DDT, 12.1%; dieldrin, 0%; deltamethrin, 24.0%; permethrin, 0%). |
0(0,0,0,0) | Details |
| 19253657 | Chen AC, He H, Temeyer KB, Jones S, Green P, Barker SC: A survey of Rhipicephalus microplus populations for mutations associated with pyrethroid resistance. J Econ Entomol. 2009 Feb;102(1):373-80. A mutation in the sodium channel gene was reported in strains highly resistant to permethrin and another mutation in an esterase gene in a strain that shows moderate resistance to the same pesticide. |
6(0,0,1,1) | Details |
| 16739412 | Kristensen M, Knorr M, Rasmussen AM, Jespersen JB: Survey of permethrin and malathion resistance in human head lice populations from Denmark. J Med Entomol. 2006 May;43(3):533-8. The frequency of the double mutation T929I-L932 F in the voltage-sensitive sodium channel gene associated with permethrin resistance was 0.95 in Danish head lice populations. |
6(0,0,1,1) | Details |
| 11296838 | Miller RJ, George JE, Guerrero F, Carpenter L, Welch JB: Characterization of acaricide resistance in Rhipicephalus sanguineus (latreille) (Acari: Ixodidae) collected from the Corozal Army Veterinary Quarantine Center, Panama. J Med Entomol. 2001 Mar;38(2):298-302. Resistance to both permethrin and DDT may result from a mutation of the sodium channel. |
6(0,0,1,1) | Details |
| 12403427 | Pruett JH, Guerrero FD, Hernandez R: Isolation and identification of an esterase from a Mexican strain of Boophilus microplus (Acari: Ixodidae). J Econ Entomol. 2002 Oct;95(5):1001-7. A strain of Mexican Boophilus microplus (Cz) collected near Coatzacoalcos, Veracruz, Mexico, exhibits a moderate, but significant, level of permethrin resistance. |
0(0,0,0,0) | Details |
| 10742517 | Jamroz RC, Guerrero FD, Pruett JH, Oehler DD, Miller RJ: Molecular and biochemical survey of acaricide resistance mechanisms in larvae from Mexican strains of the southern cattle tick, Boophilus microplus. J Insect Physiol. 2000 May 1;46(5):685-695. The electrophoretic profiles of esterase activity in protein extracts from coumaphos and permethrin-resistant strains compared to the susceptible strain revealed distinct differences, which inhibitor studies attributed to carboxylesterases. |
0(0,0,0,0) | Details |
| 20161186 | Clark JM: Determination, mechanism and monitoring of knockdown resistance in permethrin-resistant human head lice, Pediculus humanus capitis. J Asia Pac Entomol. 2009 Mar 1;12(1):1-7. Resistance to permethrin is due to knockdown resistance (kdr), which is the result of three point mutations within the alpha-subunit gene of the voltage-gated sodium channel that causes amino acid substitutions, leading to nerve insensitivity.A three-tiered resistance monitoring system has been established based on molecular resistance detection techniques. |
6(0,0,1,1) | Details |
| 8236249 | Eells JT, Rasmussen JL, Bandettini PA, Propp JM: Differences in the neuroexcitatory actions of pyrethroid insecticides and sodium channel-specific neurotoxins in rat and trout brain synaptosomes. Toxicol Appl Pharmacol. 1993 Nov;123(1):107-19. The type I pyrethroids, permethrin and NRDC 157, exhibited significantly greater intrinsic activity in trout brain synaptosomes, producing maximal membrane depolarizations that were three times greater than those observed in rat brain synaptosomes. |
4(0,0,0,4) | Details |
| 2434059 | Hong JS, Herr DW, Hudson PM, Tilson HA: Neurochemical effects of DDT in rat brain in vivo. Arch Toxicol Suppl. 1986;9:14-26. p,p'-DDT and related agents act to hold the sodium channel open once opened and this effect is believed to be responsible for neurological effects of tremor and hyperexcitability in vivo. A similar antagonism was observed for permethrin, a Type I pyrethroid believed to have a mechanism of action very similar to that of DDT. |
3(0,0,0,3) | Details |
| 17098165 | Sonoda S, Igaki C, Ashfaq M, Tsumuki H: Pyrethroid-resistant diamondback moth expresses alternatively spliced sodium channel transcripts with and without T929I mutation. Insect Biochem Mol Biol. 2006 Dec;36(12):904-10. Epub 2006 Sep 23. |
3(0,0,0,3) | Details |
| 16263118 | Usherwood PN, Vais H, Khambay BP, Davies TG, Williamson MS: Sensitivity of the Drosophila para sodium channel to DDT is not lowered by the super-kdr mutation M918T on the IIS4-S5 linker that profoundly reduces sensitivity to permethrin and deltamethrin. FEBS Lett. 2005 Nov 21;579(28):6317-25. Epub 2005 Oct 21. |
0(0,0,0,0) | Details |
| 1787887 | Eshleman AJ, Murray TF: Pyrethroid insecticides indirectly inhibit -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 -dependent influx, with a maximum inhibition of 70-82%. The sensitivity of the effect of the pyrethroid to TTX suggested an activation by pyrethroid of the voltage-dependent sodium channel. |
3(0,0,0,3) | Details |
| 18093007 | Saavedra-Rodriguez K, Urdaneta-Marquez L, Rajatileka S, Moulton M, Flores AE, Fernandez-Salas I, Bisset J, Rodriguez M, McCall PJ, Donnelly MJ, Ranson H, Hemingway J, Black WC 4th: A mutation in the voltage-gated sodium channel gene associated with pyrethroid resistance in Latin American Aedes aegypti. Insect Mol Biol. 2007 Dec;16(6):785-98. Assays on larvae from strains bearing these mutations indicated reduced nerve sensitivity to permethrin inhibition. |
2(0,0,0,2) | Details |
| 12680930 | Brengues C, Hawkes NJ, Chandre F, McCarroll L, Duchon S, Guillet P, Manguin S, Morgan JC, Hemingway J: Pyrethroid and DDT cross-resistance in Aedes aegypti is correlated with novel mutations in the voltage-gated sodium channel gene. Med Vet Entomol. 2003 Mar;17(1):87-94. Two laboratory strains, Bora (French Polynesia) and AEAE, were both susceptible to DDT and permethrin; all other strains, except Larentuka (Indonesia) and Bouake (Ivory Coast), contained individual fourth-instar larvae resistant to permethrin. |
2(0,0,0,2) | Details |
| 18538810 | Meacham CA, Brodfuehrer PD, Watkins JA, Shafer TJ: Developmentally-regulated sodium channel subunits are differentially sensitive to alpha-cyano containing pyrethroids. Toxicol Appl Pharmacol. 2008 Sep 15;231(3):273-81. Epub 2008 Apr 29. Permethrin and tetramethrin did not modify currents mediated by either subunit combination. |
2(0,0,0,2) | Details |
| 19166159 | Faraj C, Adlaoui E, Brengues C, Fontenille D, Lyagoubi M: [Resistance of Anopheles labranchiae to DDT in Morocco: identification of the mechanisms and choice of replacement insecticide]. East Mediterr Health J. 2008 Jul-Aug;14(4):776-83. An. labranchiae was susceptible to propoxur, fenitrothion and permethrin and resistant to varying degrees to DDT. |
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| 9541045 | Gotoh Y, Kawakami M, Matsumoto N, Okada Y: Permethrin emulsion ingestion: clinical manifestations and clearance of isomers. J Toxicol Clin Toxicol. 1998;36(1-2):57-61. |
0(0,0,0,0) | Details |
| 2436357 | McKillop CM, Brock JA, Oliver GJ, Rhodes C: A quantitative assessment of pyrethroid-induced paraesthesia in the guinea-pig flank model. Toxicol Lett. 1987 Mar;36(1):1-7. The aetiology of this cutaneous effect is related to the ability of pyrethroids to produce trains of nerve impulses in afferent nerves by prolonging the opening of the neuronal sodium channel. Using the guinea-pig flank model which has been developed to study this cutaneous phenomenon we have constructed dose-response curves to three structurally related pyrethroids (permethrin, cypermethrin and deltamethrin) and to a mixture of veratrum alkaloids (veratrine). |
2(0,0,0,2) | Details |
| 16032654 | Xu Q, Liu H, Zhang L, Liu N: Resistance in the mosquito, Culex quinquefasciatus, and possible mechanisms for resistance. Pest Manag Sci. 2005 Nov;61(11):1096-102. MAmCq (G0) and HAmCq (G0) were further selected in the laboratory with permethrin for one and three generations, respectively. A substitution of to (L to F) resulting from a single nucleotide polymorphism (SNP), termed the kdr mutation, in the para-homologous sodium channel gene has been reported as a very common mutation associated with pyrethroid resistance of insects. |
2(0,0,0,2) | Details |
| 17991435 | Usherwood PN, Davies TG, Mellor IR, O'Reilly AO, Peng F, Vais H, Khambay BP, Field LM, Williamson MS: Mutations in DIIS5 and the DIIS4-S5 linker of Drosophila melanogaster sodium channel define binding domains for pyrethroids and DDT. FEBS Lett. 2007 Nov 27;581(28):5485-92. Epub 2007 Nov 6. Substitutions L914I, M918T, L925I, T929I and C933A decreased deltamethrin potency, M918T, L925I and T929I decreased permethrin potency and T929I, L925I and I936V decreased fenfluthrin potency. |
2(0,0,0,2) | Details |
| 1527722 | Eells JT, Bandettini PA, Holman PA, Propp JM: Pyrethroid insecticide-induced alterations in mammalian synaptic membrane potential. J Pharmacol Exp Ther. 1992 Sep;262(3):1173-81. Both type I (permethrin) and type II (deltamethrin, cypermethrin and fenvalerate) pyrethroids produced a concentration-dependent tetrodotoxin-sensitive membrane depolarization which was stereospecific for the isomer of each pyrethroid. These data indicate that type I and type II phenoxybenzyl pyrethroids act potently and stereoselectively on the voltage-sensitive sodium channel to increase influx into synaptic terminals producing membrane depolarization and neurotransmitter release. |
2(0,0,0,2) | Details |
| 18615615 | Sonoda S, Tsukahara Y, Ashfaq M, Tsumuki H: Genomic organization of the para-sodium channel alpha-subunit genes from the pyrethroid-resistant and -susceptible strains of the diamondback moth. Arch Insect Biochem Physiol. 2008 Sep;69(1):1-12. Comparison of deduced amino acid sequences of the permethrin-resistant and -susceptible strains showed two substitutions other than kdr and super-kdr-like substitutions. |
2(0,0,0,2) | Details |
| 18304643 | Shafer TJ, Rijal SO, Gross GW: Complete inhibition of spontaneous activity in neuronal networks in vitro by deltamethrin and permethrin. Neurotoxicology. 2008 Mar;29(2):203-12. Epub 2008 Jan 19. Types I and II pyrethroid insecticides cause temporally distinct decreases in voltage-gated sodium channel (VGSC) inactivation rates that are proposed to underlie their characteristic differences in toxicity signs. |
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| 18252244 | SupYoon K, Symington SB, Hyeock Lee S, Soderlund DM, Marshall Clark J: Three mutations identified in the voltage-sensitive sodium channel alpha-subunit gene of permethrin-resistant human head lice reduce the permethrin sensitivity of house fly Vssc1 channels expressed in Xenopus oocytes. Insect Biochem Mol Biol. 2008 Mar;38(3):296-306. Epub 2007 Dec 4. |
88(1,1,2,3) | Details |
| 10612620 | Brooke BD, Hunt RH, Koekemoer LL, Dossou-Yovo J, Coetzee M: Evaluation of a polymerase chain reaction assay for detection of pyrethroid insecticide resistance in the malaria vector species of the Anopheles gambiae complex. J Am Mosq Control Assoc. 1999 Dec;15(4):565-8. A published polymerase chain reaction assay proved reliable for detecting nerve-insensitivity (kdr-type) resistant and susceptible alleles to the pyrethroid insecticide permethrin in the malaria vectors Anopheles gambiae s.s. and An. arabiensis and the nonvector species An. quadriannulatus. The assay detects pyrethroid susceptible and resistance alleles mediated by a mutation in region II of the para-type sodium channel gene, showing that resistance is conferred by pyrethroid target site insensitivity. |
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| 18260698 | Boone MD: Examining the single and interactive effects of three insecticides on amphibian metamorphosis. Environ Toxicol Chem. 2008 Jul;27(7):1561-8. I exposed tadpoles to single or multiple insecticides at approximately half the reported median lethal concentrations using insecticides that were either acetylcholinesterase inhibitors (carbaryl or malathion) or a sodium-channel disruptor (permethrin). |
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| 19960691 | Liu N, Xu Q, Li T, He L, Zhang L: Permethrin resistance and target site insensitivity in the mosquito Culex quinquefasciatus in Alabama. J Med Entomol. 2009 Nov;46(6):1424-9. Although it is possible that other mutations other than L-to-F are present in the sodium channel, resulting in permethrin resistance in these four field populations, resistance mechanisms other than target site insensitivity also must be considered. |
31(0,1,1,1) | Details |
| 18380658 | Pasay C, Arlian L, Morgan M, Vyszenski-Moher D, Rose A, Holt D, Walton S, McCarthy J: High-resolution melt analysis for the detection of a mutation associated with permethrin resistance in a population of scabies mites. Med Vet Entomol. 2008 Mar;22(1):82-8. The neuronal voltage-sensitive sodium channel (Vssc), necessary for the generation of action potentials in excitable cells, is the target of pyrethroid acaricides such as permethrin. |
31(0,1,1,1) | Details |
| 17665370 | Li AY, Chen AC, Miller RJ, Davey RB, George JE: Acaricide resistance and synergism between permethrin and amitraz against susceptible and resistant strains of Boophilus microplus (Acari: Ixodidae). Pest Manag Sci. 2007 Sep;63(9):882-9. To examine mechanisms of resistance to permethrin in these strains, the frequency of a mutated sodium channel gene was determined using a PCR assay. |
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| 18405930 | Okoye PN, Brooke BD, Koekemoer LL, Hunt RH, Coetzee M: Characterisation of DDT, pyrethroid and resistance in Anopheles funestus from Obuasi, Ghana. Trans R Soc Trop Med Hyg. 2008 Jun;102(6):591-8. Epub 2008 Apr 10. Samples of F1 progeny from each family were divided into cohorts and were either exposed to DDT and permethrin or were stored for biochemical analysis. The sodium channel gene of DDT survivors and DDT-susceptible individuals was PCR amplified and sequenced to determine whether any kdr-type mutations were present. |
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| 12615099 | Kakko I, Toimela T, Tahti H: The synaptosomal membrane bound ATPase as a target for the effects of pyrethroids, permethrin and cypermethrin. Chemosphere. 2003 May;51(6):475-80. A cellular target of pyrethroids is the sodium channel in the membrane. |
1(0,0,0,1) | Details |
| 11029667 | Ranson H, Jensen B, Vulule JM, Wang X, Hemingway J, Collins FH: Identification of a point mutation in the voltage-gated sodium channel gene of Kenyan Anopheles gambiae associated with resistance to DDT and pyrethroids. Insect Mol Biol. 2000 Oct;9(5):491-7. We cloned and sequenced a partial sodium channel cDNA from the Kenyan permethrin-resistant strain and we identified an alternative substitution to serine) at the same position, which is linked to the inheritance of permethrin resistance in the F (2) progeny of genetic crosses between susceptible and resistant individuals. |
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| 12349861 | Guerrero FD, Li AY, Hernandez R: Molecular diagnosis of pyrethroid resistance in Mexican strains of Boophilus microplus (Acari: Ixodidae). J Med Entomol. 2002 Sep;39(5):770-6. A --> amino acid mutation in the sodium channel gene S6 transmembrane segment of domain III was found to have a close association with survival of acaricide treatments containing as high as 30% permethrin. |
12(0,0,2,2) | Details |
| 19171193 | Chang C, Shen WK, Wang TT, Lin YH, Hsu EL, Dai SM: A novel amino acid substitution in a voltage-gated sodium channel is associated with knockdown resistance to permethrin in Aedes aegypti. Insect Biochem Mol Biol. 2009 Apr;39(4):272-8. Epub 2009 Jan 10. |
12(0,0,2,2) | Details |
| 15525757 | Tan J, Liu Z, Wang R, Huang ZY, Chen AC, Gurevitz M, Dong K: Identification of amino acid residues in the insect sodium channel critical for pyrethroid binding. Mol Pharmacol. 2005 Feb;67(2):513-22. Epub 2004 Nov 3. Here, we show that an F-to-I substitution at 1519 (F1519I) in segment 6 of domain III (IIIS6) abolished the sensitivity of the cockroach sodium channel expressed in Xenopus laevis oocytes to all eight structurally diverse pyrethroids examined, including permethrin and deltamethrin. |
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| 14570139 | Guerrero FD, Pruett JH, Li AY: Molecular and biochemical diagnosis of esterase-mediated pyrethroid resistance in a Mexican strain of Boophilus microplus (Acari: Ixodidae). Exp Appl Acarol. 2002;28(1-4):257-64. Permethrin hydrolysis assays and esterase activity gels indicated enhanced esterase-mediated metabolic detoxification in the Cz strain, while one other pyrethroid resistant strain, SF, and two pyrethroid susceptible strains had lower levels of permethrin hydrolysis. Results from assays using a PCR-based test to detect a pyrethroid target site resistance-associated mutation in the tick sodium channel gene found only low levels of mutations in the Cz strain, while the SF strain had a high level of the mutated sodium channel alleles. |
1(0,0,0,1) | Details |
| 14500748 | Vais H, Atkinson S, Pluteanu F, Goodson SJ, Devonshire AL, Williamson MS, Usherwood PN: Mutations of the para sodium channel of Drosophila melanogaster identify putative binding sites for pyrethroids. Mol Pharmacol. 2003 Oct;64(4):914-22. Channels were expressed in Xenopus laevis oocytes and the effects of the pyrethroids permethrin (type I) and deltamethrin (type II) on Na+ currents were investigated using voltage clamp. |
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| 9280307 | Vais H, Williamson MS, Hick CA, Eldursi N, Devonshire AL, Usherwood PN: Functional analysis of a rat sodium channel carrying a mutation for insect knock-down resistance (kdr) to pyrethroids. FEBS Lett. 1997 Aug 18;413(2):327-32. An alpha-subunit of rat brain type II sodium channel containing this mutation has been expressed and its sensitivity to permethrin compared with that of the wild-type channel. |
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| 15843294 | Coleman CI, Gillespie EL, White CM: Probable topical permethrin-induced neck dystonia. . Pharmacotherapy. 2005 Mar;25(3):448-50. The mechanism behind these adverse effects may be related to permethrin's ability to delay sodium channel closure within nerve cells. |
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| 9236205 | Warmke JW, Reenan RA, Wang P, Qian S, Arena JP, Wang J, Wunderler D, Liu K, Kaczorowski GJ, Van der Ploeg LH, Ganetzky B, Cohen CJ: Functional expression of Drosophila para channels. J Gen Physiol. 1997 Aug;110(2):119-33. The Drosophila para sodium channel alpha subunit was expressed in Xenopus oocytes alone and in combination with tipE, a putative Drosophila sodium channel accessory subunit. However, the pharmacology of these channels differs from that of vertebrate channels: (a) toxin II from Anemonia sulcata, which slows inactivation, binds to Para and some mammalian channels with similar affinity (Kd congruent with 10 nM), but this toxin causes a 100-fold greater decrease in the rate of inactivation of Para/TipE than of mammalian channels; (b) Para channels are > 10-fold more sensitive to block by tetrodotoxin; and (c) modification by the pyrethroid insecticide permethrin is > 100-fold more potent for Para than for rat brain type IIA channels. |
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