| Name | sodium channel (protein family or complex) |
|---|---|
| Synonyms | Sodium channel |
| Name | deltamethrin |
|---|---|
| CAS |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 2546560 | Clark JM, Brooks MW: Role of ion channels and intraterminal homeostasis in the action of deltamethrin at presynaptic nerve terminals. Biochem Pharmacol. 1989 Jul 15;38(14):2233-45. Since tetrodotoxin is a specific sodium channel blocker, deltamethrin may be enhancing [3H] release by increasing the uptake of Ca2 via other voltage-gated channels (e.g. or exchange mechanisms in addition to its action at voltage-gated channels. |
7(0,0,1,2) | Details |
| 12097481 | Tan J, Liu Z, Nomura Y, Goldin AL, Dong K: Alternative splicing of an insect sodium channel gene generates pharmacologically distinct channels. J Neurosci. 2002 Jul 1;22(13):5300-9. Furthermore, these two functional splicing variants exhibited a striking difference in sensitivity to a pyrethroid insecticide, deltamethrin. |
6(0,0,0,6) | Details |
| 17574382 | Watkins JA, Meacham CA, Crofton KM, Shafer TJ: Concentration-dependent accumulation of [3H]-deltamethrin in sodium channel Nav1.2/beta1 expressing Xenopus laevis oocytes. Toxicol In Vitro. 2007 Dec;21(8):1672-7. Epub 2007 May 16. |
6(0,0,1,1) | Details |
| 2885137 | Matsumura F: Deltamethrin-induced changes in synaptosomal transport of 3H- in the squid optic lobes. Comp Biochem Physiol C. 1987;87(1):31-5. Only a part of such a deltamethrin effect was due to its effect on the sodium channel. |
6(0,0,1,1) | 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 |
| 1281937 | Narahashi T, Frey JM, Ginsburg KS, Roy ML: and -activated channels as the targets of pyrethroids and cyclodienes. Toxicol Lett. 1992 Dec;64-65 Spec No:429-36. The type I pyrethroid allethrin and the type II pyrethroid deltamethrin were both effective in prolonging the current in the TXX-resistant sodium channel but had only a small effect on the TTX-sensitive sodium channel. |
6(0,0,1,1) | Details |
| 2419769 | Brodie ME, Opacka J: Dissociation between circling behaviour and striatal activity following unilateral deltamethrin administration to rats. Naunyn Schmiedebergs Arch Pharmacol. 1985 Dec;331(4):341-6. These findings also indicate that a degree of selectivity exists in the action of deltamethrin, a sodium channel toxin that might be expected to act on all neuronal systems within the SN or VTN or equally at other sites within the basal ganglia associated with circling behaviour. |
6(0,0,1,1) | Details |
| 2433987 | Narahashi T: Toxins that modulate the sodium channel gating mechanism. . Ann N Y Acad Sci. 1986;479:133-51. Type II pyrethroids which contain an alpha-cyano group (e.g., deltamethrin, cyphenothrin, and fenvalerate) exert effects on channels qualitatively similar to those of type I pyrethroids. |
5(0,0,0,5) | 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. Type II (deltamethrin, cypermethrin) pyrethroids produced similar depolarizing responses in rat and trout synaptosomes; however, the 1R-cis-alpha R isomer of deltamethrin, which had no effect on membrane potential in rat synaptosomes, depolarized trout synaptosomes. |
4(0,0,0,4) | Details |
| 2423935 | Bloomquist JR, Miller TA: Sodium channel neurotoxins as probes of the knockdown resistance mechanism. Neurotoxicology. 1986 Spring;7(1):217-23. The pyrethroid-resistant strains kdr and super-kdr, which are thought to have rediced neural sensitivity to pyrethroids, displayed 28-fold and greater than 909-fold resistance to deltamethrin when compared to the pyrethroid-susceptible NAIDM strain. |
4(0,0,0,4) | Details |
| 2547381 | Ishikawa Y, Charalambous P, Matsumura F: Modification by pyrethroids and DDT of phosphorylation activities of rat brain sodium channel. Biochem Pharmacol. 1989 Aug 1;38(15):2449-57. Phosphorylation of the alpha-subunit was induced by depolarization, and this process was inhibited by 10 (-6) to 10 (-10) M 1R-deltamethrin, but not by 1S-deltamethrin, the latter being an inactive enantiomer of the former. |
4(0,0,0,4) | Details |
| 8107074 | Grant AO, Wendt DJ, Zilberter Y, Starmer CF: Kinetics of interaction of disopyramide with the cardiac sodium channel: fast dissociation from open channels at normal rest potentials. J Membr Biol. 1993 Nov;136(2):199-214. Exposure of cells to the pyrethrin toxins deltamethrin or fenvalrate caused at least a tenfold increase in mean open time, and prominent tail currents could be recorded at the normal resting potential. |
3(0,0,0,3) | Details |
| 15657957 | Brun-Barale A, Bouvier JC, Pauron D, Berge JB, Sauphanor B: Involvement of a sodium channel mutation in pyrethroid resistance in Cydia pomonella L, and development of a diagnostic test. Pest Manag Sci. 2005 Jun;61(6):549-54. We have studied two susceptible strains (S and Sv) and two resistant strains (Rt and Rv) of C pomonella that exhibited 4- and 80-fold resistance ratios to deltamethrin, respectively. |
3(0,0,0,3) | 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 |
| 18528710 | Aguilar-Tipacamu G, Miller RJ, Hernandez-Ortiz R, Rodriguez-Vivas RI, Vasquez-Pelaez C, Garcia-Vazquez Z, Olvera-Valencia F, Rosario-Cruz R: Inheritance of pyrethroid resistance and a sodium channel gene mutation in the cattle tick Boophilus microplus. Parasitol Res. 2008 Aug;103(3):633-9. Epub 2008 Jun 5. The reciprocal crosses show a predominance of the heterozygote genotype, in agreement with the significant decrease of the acaricide resistance to cypermethrin, deltamethrin, and flumethrin. |
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. Selection experiments, one with deltamethrin on a field strain from Santiago de Cuba and another with permethrin on a strain from Isla Mujeres, Mexico rapidly increased the frequency of the Iso1016 allele. |
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. Juvenile rats have been reported to be more sensitive to the acute effects of the pyrethroid deltamethrin than adults. |
2(0,0,0,2) | Details |
| 19565267 | Rosario-Cruz R, Guerrero FD, Miller RJ, Rodriguez-Vivas RI, Tijerina M, Dominguez-Garcia DI, Hernandez-Ortiz R, Cornel AJ, McAbee RD, Alonso-Diaz MA: Molecular survey of pyrethroid resistance mechanisms in Mexican field populations of Rhipicephalus (Boophilus) microplus. Parasitol Res. 2009 Oct;105(4):1145-53. Epub 2009 Jun 30. Larval packet test (LPT), knock-down (kdr) PCR allele-specific assay (PASA) and esterase activity assays were conducted in tick populations for cypermethrin, flumethrin and deltamethrin. However a significant correlation (p < 0.01) was found between the presence of the sodium channel mutation, and resistance to SP s as measured by PASA and LPT respectively. |
2(0,0,0,2) | 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 |
| 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 |
| 15337272 | Choi JS, Soderlund DM: Cyclosporin A and deltamethrin block the downregulation of Nav1.8 channels expressed in Xenopus oocytes. Neurosci Lett. 2004 Sep 9;367(3):389-93. The Nav1.8 sodium channel isoform, expressed in sensory neurons and implicated in pain responses, is known to be upregulated in Xenopus oocytes by agents that activate protein kinase A. |
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 |
| 10469251 | Martinez-Torres D, Foster SP, Field LM, Devonshire AL, Williamson MS: A sodium channel point mutation is associated with resistance to DDT and pyrethroid insecticides in the peach-potato aphid, Myzus persicae (Sulzer) (Hemiptera: Aphididae). Insect Mol Biol. 1999 Aug;8(3):339-46. The inferred presence of kdr-type resistance in the four E4 clones was subsequently confirmed by bioassays that showed this to be the primary mechanism of resistance to deltamethrin and DDT, although the esterase-based mechanism also contributes to the overall level of deltamethrin resistance. |
2(0,0,0,2) | Details |
| 10528405 | Zlotkin E, Devonshire AL, Warmke JW: The pharmacological flexibility of the insect voltage gated sodium channel: toxicity of AaIT to knockdown resistant (kdr) flies. Insect Biochem Mol Biol. 1999 Oct;29(10):849-53. The para ts2 Drosophila strain, with a point of mutation in domain I of the para gene conferring a 6-fold resistance to deltamethrin also showed about 15-fold tolerance to AaIT. |
2(0,0,0,2) | Details |
| 11416227 | Li WI, Berman FW, Okino T, Yokokawa F, Shioiri T, Gerwick WH, Murray TF: Antillatoxin is a marine cyanobacterial toxin that potently activates voltage-gated channels. Proc Natl Acad Sci U S A. 2001 Jun 19;98(13):7599-604. Additional, more direct, evidence for an interaction with voltage-gated channels was derived from the ATX-induced allosteric enhancement of [3H] batrachotoxin binding to neurotoxin site 2 of the alpha subunit of the sodium channel. Positive allosteric interactions were not observed between ATX and either alpha-scorpion toxin or the pyrethroid deltamethrin. |
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. |
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 |
| 2440147 | Brown LD, Narahashi T: Activity of tralomethrin to modify the nerve membrane sodium channel. . Toxicol Appl Pharmacol. 1987 Jul;89(3):305-13. Deltamethrin is a potent type II pyrethroid insecticide which can modify sodium channel gating kinetics in nerve membranes. |
195(2,3,3,5) | Details |
| 16039402 | LePage KT, Goeger D, Yokokawa F, Asano T, Shioiri T, Gerwick WH, Murray TF: The lipopeptide kalkitoxin interacts with voltage-sensitive channels in cerebellar granule neurons. Toxicol Lett. 2005 Aug 14;158(2):133-9. Epub 2005 Apr 9. The marine neurotoxin kalkitoxin, a thiazoline-containing lipid derived from the pantropical marine cyanobacterium Lyngbya majuscula, was assayed for interaction with the tetrodotoxin-sensitive, voltage-sensitive sodium channel (TTX-VSSC) in cerebellar granule neuron cultures (CGN). Although kalkitoxin was without effect on the basal binding of [3H] BTX to intact cerebellar granule neurons, in the presence of the positive allosteric modulator, deltamethrin, [3H] BTX binding was inhibited by KTx-7 in a concentration-dependent manner (11.9 nM [IC50=3.8-37.2 nM, 95% CI]). |
1(0,0,0,1) | Details |
| 10662599 | Forshaw PJ, Lister T, Ray DE: The role of voltage-gated channels in type II pyrethroid insecticide poisoning. Toxicol Appl Pharmacol. 2000 Feb 15;163(1):1-8. Pyrethroids act on mammalian channels, but we have previously shown that low concentrations of the type II pyrethroid deltamethrin also decrease the open channel probability (P (o)) of voltage-gated channels. This effect would be expected to amplify the sodium channel-mediated signs of poisoning produced by pyrethroids. |
1(0,0,0,1) | Details |
| 2449265 | Ruigt GS, Neyt HC, Van der Zalm JM, Van den Bercken J: Increase of current after pyrethroid insecticides in mouse neuroblastoma cells. Brain Res. 1987 Dec 29;437(2):309-22. The effects of 4 different pyrethroid insecticides on sodium channel gating in internally perfused, cultured mouse neuroblastoma cells (N1E-115) were studied using the suction pipette, voltage clamp technique. The rate of decay of the slow tail current strongly depended on pyrethroid structure and increased in the order deltamethrin, cyphenothrin, fenfluthrin and phenothrin. |
1(0,0,0,1) | Details |
| 16180929 | Bradberry SM, Cage SA, Proudfoot AT, Vale JA: Poisoning due to pyrethroids. Toxicol Rev. 2005;24(2):93-106. In tropical countries mosquito nets are commonly soaked in solutions of deltamethrin as part of antimalarial strategies. Pyrethroids are some 2250 times more toxic to insects than mammals because insects have increased sodium channel sensitivity, smaller body size and lower body temperature. |
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 |
| 11714887 | Tabarean IV, Narahashi T: Kinetics of modulation of tetrodotoxin-sensitive and tetrodotoxin-resistant channels by tetramethrin and deltamethrin. J Pharmacol Exp Ther. 2001 Dec;299(3):988-97. Slowing of the kinetics of sodium channel activation by deltamethrin was revealed even after the fast inactivation had been removed by papain. |
163(2,2,2,3) | Details |
| 11886779 | Tan J, Liu Z, Tsai TD, Valles SM, Goldin AL, Dong K: Novel sodium channel gene mutations in Blattella germanica reduce the sensitivity of expressed channels to deltamethrin. Insect Biochem Mol Biol. 2002 Apr;32(4):445-54. |
120(1,2,3,5) | Details |
| 11886774 | Liu Z, Tan J, Valles SM, Dong K: Synergistic interaction between two cockroach sodium channel mutations and a tobacco budworm sodium channel mutation in reducing channel sensitivity to a pyrethroid insecticide. Insect Biochem Mol Biol. 2002 Apr;32(4):397-404. We found that the V409M mutation alone modified the gating properties of the sodium channel and reduced channel sensitivity to deltamethrin by 10-fold. |
116(1,2,2,6) | Details |
| 1325250 | Brown LD, Narahashi T: Modulation of nerve membrane sodium channel activation by deltamethrin. . Brain Res. 1992 Jul 3;584(1-2):71-6. |
88(1,1,2,3) | Details |
| 6302535 | Narahashi T: Cellular and molecular mechanisms of action of insecticides: neurophysiological approach. Neurobehav Toxicol Teratol. 1982 Nov-Dec;4(6):753-8. Type II pyrethroids as represented by cyphenothrin, deltamethrin and fenvalerate which contain a cyano group at the alpha-carbon cause nerve membrane depolarization and block leading to paralysis of the animal. Thus, it is concluded that the site of action of pyrethroids is the sodium channel, and that pyrethroids interact with the channel macromolecules that control the gating mechanism. |
1(0,0,0,1) | Details |
| 2542881 | Chinn K, Narahashi T: Temperature-dependent subconducting states and kinetics of deltamethrin-modified channels of neuroblastoma cells. Pflugers Arch. 1989 Apr;413(6):571-9. The decay of the summed modified single sodium channel currents at -30 mV was expressed by a single exponential function at 11 degrees C, and by two exponential functions at room temperature. |
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. |
1(0,0,0,1) | Details |
| 16007969 | Yaicharoen R, Kiatfuengfoo R, Chareonviriyaphap T, Rongnoparut P: Characterization of deltamethrin resistance in field populations of Aedes aegypti in Thailand. J Vector Ecol. 2005 Jun;30(1):144-50. The partial cDNA sequence of the para-type voltage-dependent sodium channel (IIS4-IIS6) was determined for BKH and PSC populations. |
1(0,0,0,1) | Details |
| 20301216 | Zhu F, Wigginton J, Romero A, Moore A, Ferguson K, Palli R, Potter MF, Haynes KF, Palli SR: Widespread distribution of knockdown resistance mutations in the bed bug, Cimex lectularius (Hemiptera: Cimicidae), populations in the United States. Arch Insect Biochem Physiol. 2010 Apr;73(4):245-57. These data suggest that deltamethrin resistance conferred by target-site insensitivity of sodium channel is widely spread in bed bug populations across the United States. |
88(1,1,2,3) | Details |
| 2441036 | Chinn K, Narahashi T: Stabilization of sodium channel states by deltamethrin in mouse neuroblastoma cells. J Physiol. 1986 Nov;380:191-207. The study was aimed at determining how the effects of deltamethrin at the whole cell level would be reflected in the modified properties of single sodium channel currents. |
87(1,1,2,2) | Details |
| 11456334 | Motomura H, Narahashi T: Interaction of tetramethrin and deltamethrin at the single sodium channel in rat hippocampal neurons. Neurotoxicology. 2001 Jun;22(3):329-39. |
83(1,1,1,3) | Details |
| 2452970 | Bloomquist JR, Soderlund DM: Pyrethroid insecticides and DDT modify alkaloid-dependent sodium channel activation and its enhancement by sea anemone toxin. Mol Pharmacol. 1988 May;33(5):543-50. The effects of saturating concentrations of DDT [1,1,1-trichloro-2,2-bis (p-chlorophenyl) ethane] and the pyrethroid insecticides cismethrin and deltamethrin on alkaloid-dependent activation of the voltage-sensitive sodium channel were studied using measurements of 22Na+ uptake into mouse brain synaptosomes. |
83(1,1,1,3) | 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 |
| 9495855 | Tabarean IV, Narahashi T: Potent modulation of tetrodotoxin-sensitive and tetrodotoxin-resistant channels by the type II pyrethroid deltamethrin. J Pharmacol Exp Ther. 1998 Mar;284(3):958-65. These results suggest that the deltamethrin and tetramethrin share a binding site on the sodium channel and that the slow onset and offset of deltamethrin action are controlled by the rates at which deltamethrin moves and unbinds from the membrane lipid phase rather than by the rate of deltamethrin binding to the sodium channel site. |
81(1,1,1,1) | Details |
| 16325806 | Dekker LV, Daniels Z, Hick C, Elsegood K, Bowden S, Szestak T, Burley JR, Southan A, Cronk D, James IF: Analysis of human Nav1.8 expressed in SH-SY5Y neuroblastoma cells. Eur J Pharmacol. 2005 Dec 28;528(1-3):52-8. Epub 2005 Dec 2. Both voltage-activated and deltamethrin-activated human Nav1.8 were inhibited by the sodium channel blockers BIII 890 CL, NW-1029, and mexiletine. |
31(0,1,1,1) | 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. |
10(0,0,1,5) | 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 |
| 14769548 | Vickery RG, Amagasu SM, Chang R, Mai N, Kaufman E, Martin J, Hembrador J, O'Keefe MD, Gee C, Marquess D, Smith JA: Comparison of the pharmacological properties of rat Na (V) 1.8 with rat Na (V) 1.2a and human Na (V) 1.5 voltage-gated sodium channel subtypes using a membrane potential sensitive dye and FLIPR. Receptors Channels. 2004;10(1):11-23. In contrast, the type II pyrethroids deltamethrin and fenvalerate evoked direct depolarization of Na (v) 1.8-F-11 and Na (v) 1.5-293-EBNA cells. |
1(0,0,0,1) | 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 |
| 16431283 | Du Y, Liu Z, Nomura Y, Khambay B, Dong K: An in segment 3 of domain III (IIIS3) of the cockroach sodium channel contributes to the low pyrethroid sensitivity of an alternative splice variant. Insect Biochem Mol Biol. 2006 Feb;36(2):161-8. Epub 2005 Dec 20. In a previous study, we showed that two alternative exons (G1 and G2 encoding IIIS3-S4) were involved in the differential sensitivity of two cockroach sodium channel splice variants, BgNa (v) 1-1 and BgNa (v) 2-1 (previously called KD1 and KD2), to deltamethrin, a pyrethroid insecticide (Tan, et al., 2002b. |
9(0,0,1,4) | Details |
| 16465743 | Rosario-Cruz R, Guerrero FD, Miller RJ, Rodriguez-Vivas RI, Dominguez-Garcia DI, Cornel AJ, Hernandez-Ortiz R, George JE: Roles played by esterase activity and by a sodium channel mutation involved in pyrethroid resistance in populations of Boophilus microplus (Acari: Ixodidae) collected from Yucatan, Mexico. J Med Entomol. 2005 Nov;42(6):1020-5. It was concluded that within the B. microplus populations studied, resistance to flumethrin, deltamethrin, or cypermethrin was because of the novel sodium channel mutation --> amino acid substitution in the S6 transmembrane segment of domain III), and there was a correlation between tick mortality by pyrethroid exposure (larval survival) and the presence of R allele. |
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| 18448863 | Cao Z, George J, Gerwick WH, Baden DG, Rainier JD, Murray TF: Influence of lipid-soluble gating modifier toxins on influx in neocortical neurons. J Pharmacol Exp Ther. 2008 Aug;326(2):604-13. Epub 2008 Apr 30. The rank order of efficacy of sodium channel gating modifiers was brevetoxin (PbTx)-1 > PbTx-desoxydioxolane > batrachotoxin > antillatoxin > PbTx-2 = PbTx-3 > PbTx-3alpha-naphthoate > veratridine > deltamethrin > aconitine > gambierol. |
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| 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%). |
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| 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. |
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| 2458984 | Ogata N, Vogel SM, Narahashi T: Lindane but not deltamethrin blocks a component of -activated channels. FASEB J. 1988 Oct;2(13):2895-900. |
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| 2702491 | Gilbert ME, Mack CM, Crofton KM: Pyrethroids and enhanced inhibition in the hippocampus of the rat. Brain Res. 1989 Jan 16;477(1-2):314-21. The GABAergic properties of the pyrethroids were assessed by examining paired pulse inhibition before and after oral treatment with 20 mg/kg of cismethrin (Type I), 20 mg/kg of fenvalerate, or 10 mg/kg of deltamethrin (Type IIs). |
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| 19058634 | Yoon KS, Kwon DH, Strycharz JP, Hollingsworth CS, Lee SH, Clark JM: Biochemical and molecular analysis of deltamethrin resistance in the common bed bug (Hemiptera: Cimicidae). J Med Entomol. 2008 Nov;45(6):1092-101. |
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