| Name | sodium channel (protein family or complex) |
|---|---|
| Synonyms | Sodium channel |
| Name | fenvalerate |
|---|---|
| CAS | cyano(3-phenoxyphenyl)methyl 4-chloro-α-(1-methylethyl)benzeneacetate |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 17257205 | Grubor VD, Heckel DG: Evaluation of the role of CYP6B cytochrome P450s in pyrethroid resistant Australian Helicoverpa armigera. Insect Mol Biol. 2007 Feb;16(1):15-23. The AN02 strain of Helicoverpa armigera from eastern Australia exhibits 50-fold, PBO-suppressible resistance to the pyrethroid insecticide fenvalerate. In evaluating the cytochrome P450 genes CYP6B7, CYP6B6, and CYP6B2 as candidates for RFen1, we found that they occur in a tandem array in the genome, next to the gene encoding the para-type sodium channel; the target of pyrethroid insecticides. |
1(0,0,0,1) | 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. Tail currents for the remaining compounds (bifenthrin, fenpropathrin, fenvalerate and tefluthrin) were monoexponential and decayed with kinetics intermediate between these extremes. |
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 |
| 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 |
| 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 |
| 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). |
0(0,0,0,0) | Details |
| 8720856 | Song JH, Nagata K, Tatebayashi H, Narahashi T: Interactions of tetramethrin, fenvalerate and DDT at the sodium channel in rat dorsal root ganglion neurons. Brain Res. 1996 Feb 5;708(1-2):29-37. |
164(2,2,2,4) | Details |
| 16475981 | O'Reilly AO, Khambay BP, Williamson MS, Field LM, Wallace BA, Davies TG: Modelling insecticide-binding sites in the voltage-gated sodium channel. . Biochem J. 2006 Jun 1;396(2):255-63. A homology model of the housefly voltage-gated sodium channel was developed to predict the location of binding sites for the insecticides fenvalerate, a synthetic pyrethroid, and DDT an early generation organochlorine. |
83(1,1,1,3) | Details |
| 11488435 | Kamei J, Sasaki M, Zushida K, Morita K, Tanaka S: Nociception and allodynia/hyperalgesia induced by intrathecal administration of fenvalerate. Jpn J Pharmacol. 2001 Jul;86(3):336-41. The intrathecal injection of fenvalerate, a sodium channel activator, at doses of 0.01 to 3 microg, dose-dependently induced the duration of a characteristic behavioral syndrome mainly consisting of reciprocal hind limb scratching directed towards caudal parts of the body and biting or licking of the hind legs in mice. |
32(0,1,1,2) | Details |
| 3404444 | Eells JT, Dubocovich ML: Pyrethroid insecticides evoke neurotransmitter release from rabbit striatal slices. J Pharmacol Exp Ther. 1988 Aug;246(2):514-21. The release of [3H] and [3H] by fenvalerate was modulated by D2 receptor activation and antagonized completely by the sodium channel blocker, tetrodotoxin. |
31(0,1,1,1) | Details |
| 12383951 | Kamei J, Iguchi E, Sasaki M, Zushida K, Morita K, Tanaka S: Modification of the fenvalerate-induced nociceptive response in mice by diabetes. Brain Res. 2002 Sep 6;948(1-2):17-23. The intrathecal (i.t.) or intraplantar (i.pl.) injection of fenvalerate, a sodium channel activator, induced a characteristic behavioral syndrome mainly consisting of reciprocal hind limb scratching directed towards caudal parts of the body and biting or licking of the hind legs in both non-diabetic and diabetic mice. |
31(0,1,1,1) | Details |
| 2434060 | Narahashi T: Nerve membrane ionic channels as the target of toxicants. Arch Toxicol Suppl. 1986;9:3-13. Fenvalerate, a cyano-containing type II pyrethroid, prolongs the sodium channel open time much more drastically than tetramethrin. |
8(0,0,1,3) | Details |
| 8386311 | Salgado VL, Narahashi T: Immobilization of sodium channel gating charge in crayfish giant axons by the insecticide fenvalerate. Mol Pharmacol. 1993 Apr;43(4):626-34. |
7(0,0,1,2) | Details |
| 2549473 | Salgado VL, Herman MD, Narahashi T: Interactions of the pyrethroid fenvalerate with nerve membrane channels: temperature dependence and mechanism of depolarization. Neurotoxicology. 1989 Spring;10(1):1-14. Even when applied directly to the internal face of the membrane, the effect of fenvalerate on the sodium channel developed slowly, taking more than 90 min to reach its final level. |
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 |
| 11860918 | Wang X, Xiao H, Dai X, Liu X, Yu X, Wu J: [Effects of phoxim and fenvalerate on TTX-S and TTX-R channels in the DRG neurons of adult rat]. Zhonghua Yu Fang Yi Xue Za Zhi. 2000 May;34(3):136-9. RESULTS: The inactivation of TTX-R sodium channel was obviously slowed down by Fen. |
4(0,0,0,4) | Details |
| 1336116 | Gusovsky F, Padgett WL, Creveling CR, Daly JW: Interaction of pumiliotoxin B with an "alkaloid-binding domain" on the voltage-dependent sodium channel. Mol Pharmacol. 1992 Dec;42(6):1104-8. Both a type I pyrethroid (allethrin) and a type II pyrethroid (fenvalerate) inhibit PTX-B- and PTX-B/alpha-scorpion toxin-mediated 22Na+ influx. |
3(0,0,0,3) | 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 |
| 15528843 | Kamei J, Saitoh A, Tamura N: Effect of mexiletine on fenvalerate-induced nociceptive response in diabetic mice. J Pharmacol Sci. 2004 Nov;96(3):280-5. Epub 2004 Nov 5. This effect may be, at least in part, mediated by the inhibition of TTX-R sodium channel-mediated nociceptive transmission in the spinal cord. |
1(0,0,0,1) | Details |
| 7780863 | Nozaki S, Takahashi M, Hashimoto K: Effect of pyrethroid (allethrin and fenvalerate) on excitability changes following nerve impulse. Sangyo Eiseigaku Zasshi. 1995 Jan;37(1):5-8. The difference has been reported to depend on the effect on the sodium channel opening time. |
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. 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. The finding of insecticidal activity in a group of phenylacetic 3-phenoxybenzyl esters, which lacked the cyclopropane ring but contained the alpha-cyano group (and hence were type II pyrethroids) led to the development of fenvalerate and related compounds. |
1(0,0,0,1) | Details |