| Name | chloride channel (protein family or complex) |
|---|---|
| Synonyms | chloride channel |
| Name | fipronil |
|---|---|
| CAS |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 17615118 | Narahashi T, Zhao X, Ikeda T, Nagata K, Yeh JZ: Differential actions of insecticides on target sites: basis for selective toxicity. Hum Exp Toxicol. 2007 Apr;26(4):361-6. Fipronil, a phenylpyrazole, is known to act on the gamma-aminobutyric acid receptor to block the chloride channel. |
162(2,2,2,2) | Details |
| 8546445 | Bloomquist JR: Ion channels as targets for insecticides. Annu Rev Entomol. 1996;41:163-90. The arylheterocycles (e.g. endosulfan and fipronil) are potent convulsants and insecticides that block the -gated chloride channel. |
81(1,1,1,1) | Details |
| 14637375 | Ikeda T, Zhao X, Kono Y, Yeh JZ, Narahashi T: Fipronil modulation of -induced currents in cockroach thoracic ganglion neurons. Neurotoxicology. 2003 Dec;24(6):807-15. We studied the effects of fipronil on the inhibitory glutamate receptor-chloride channel complex, which is found only in invertebrates. |
81(1,1,1,1) | Details |
| 11503069 | Schlenk D, Huggett DB, Allgood J, Bennett E, Rimoldi J, Beeler AB, Block D, Holder AW, Hovinga R, Bedient P: Toxicity of fipronil and its degradation products to Procambarus sp.: field and laboratory studies. Arch Environ Contam Toxicol. 2001 Oct;41(3):325-32. An arthropod-selective insecticide, fipronil blocks the -gated chloride channel and is unique in that several of its degradation products have been indicated to be equal or more potent than fipronil. |
81(1,1,1,1) | Details |
| 16336717 | Garcia del Pino F, Jove M: Compatibility of entomopathogenic nematodes with fipronil. . J Helminthol. 2005 Dec;79(4):333-7. The survival and infectivity of infective juveniles (IJs) of three species of entomopathogenic nematodes, Steinernema carpocapsae Weiser, S. arenarium (Artyukhovsky) (Rhabditida: Steinernematidae) and Heterorhabditis bacteriophora Poinar (Rhabditida: Heterorhabditidae), were determined after exposure to different concentrations (250, 500, 1000 and 2000 ppm) of fipronil, an insecticide acting on the GABA receptors to block the chloride channel. |
81(1,1,1,1) | Details |
| 11677140 | Sirisoma NS, Ratra GS, Tomizawa M, Casida JE: Fipronil-based photoaffinity probe for Drosophila and human beta 3 GABA receptors. Bioorg Med Chem Lett. 2001 Nov 19;11(22):2979-81. Modification of the major insecticide fipronil (1) by replacing three pyrazole substituents for both cyano and amino and trifluoromethyldiazirinyl for trifluoromethylsulfinyl) gives a candidate photoaffinity probe (3) of high potency (IC (50) 2-28 nM) in blocking the chloride channel of Drosophila and human beta 3 GABA receptors. |
81(1,1,1,1) | Details |
| 9860498 | Hainzl D, Cole LM, Casida JE: Mechanisms for selective toxicity of fipronil insecticide and its sulfone metabolite and desulfinyl photoproduct. Chem Res Toxicol. 1998 Dec;11(12):1529-35. Fipronil, an N-phenylpyrazole with a trifluoromethylsulfinyl substituent, initiated the second generation of insecticides acting at the (GABA) receptor to block the chloride channel. |
81(1,1,1,1) | Details |
| 8917493 | Hainzl D, Casida JE: Fipronil insecticide: novel photochemical desulfinylation with retention of neurotoxicity. Proc Natl Acad Sci U S A. 1996 Nov 12;93(23):12764-7. The persistence of this photoproduct and its high neuroactivity, resulting from blocking the lambda-aminobutyric acid-gated chloride channel, suggest that it may be a significant contributor to the effectiveness of fipronil. |
32(0,1,1,2) | Details |
| 7582519 | Hosie AM, Baylis HA, Buckingham SD, Sattelle DB: Actions of the insecticide fipronil, on dieldrin-sensitive and- resistant GABA receptors of Drosophila melanogaster. Br J Pharmacol. 1995 Jul;115(6):909-12. Blocking actions of the novel insecticide, fipronil, were examined on responses recorded from Xenopus oocytes expressing either wild type (dieldrin-sensitive) or mutant (dieldrin-resistant) forms of the Drosophila melanogaster -gated chloride channel homo-oligomer, RDL (the product of the resistance to dieldrin locus: Rdl). 2. |
31(0,1,1,1) | Details |
| 17201770 | Eguchi Y, Ihara M, Ochi E, Shibata Y, Matsuda K, Fushiki S, Sugama H, Hamasaki Y, Niwa H, Wada M, Ozoe F, Ozoe Y: Functional characterization of Musca - and -gated channels expressed independently and coexpressed in Xenopus oocytes. Insect Mol Biol. 2006 Dec;15(6):773-83. Both channels were ion-permeable, and the MdRdl channel was more sensitive to chloride channel blockers, such as gamma-hexachlorocyclohexane (gamma-HCH), fipronil and picrotoxinin, than the MdGluCl-alpha channel. |
7(0,0,1,2) | Details |
| 11250875 | Horoszok L, Raymond V, Sattelle DB, Wolstenholme AJ: GLC-3: a novel fipronil and BIDN-sensitive, but picrotoxinin-insensitive, -gated chloride channel subunit from Caenorhabditis elegans. Br J Pharmacol. 2001 Mar;132(6):1247-54. |
7(0,0,1,2) | Details |
| 15641641 | Mohamed F, Senarathna L, Percy A, Abeyewardene M, Eaglesham G, Cheng R, Azher S, Hittarage A, Dissanayake W, Sheriff MH, Davies W, Buckley NA, Eddleston M: Acute human self-poisoning with the N-phenylpyrazole insecticide fipronil--a GABAA-gated chloride channel blocker. J Toxicol Clin Toxicol. 2004;42(7):955-63. |
6(0,0,1,1) | Details |
| 14635176 | Bloomquist JR: channels as tools for developing selective insecticides. Arch Insect Biochem Physiol. 2003 Dec;54(4):145-56. The (1)) receptor/ ionophore complex is the primary site of action for a number of currently used insecticides, such as lindane, endosulfan, and fipronil. These compounds act as antagonists by stabilizing nonconducting conformations of the chloride channel. |
5(0,0,0,5) | Details |
| 12770577 | Zheng Y, Priest B, Cully DF, Ludmerer SW: RdlDv, a novel -gated chloride channel gene from the American dog tick Dermacentor variabilis. Insect Biochem Mol Biol. 2003 Jun;33(6):595-9. When expressed in Xenopus oocytes, RdlDv produces -activated currents blocked by the known insecticides and RDL antagonists fipronil and picrotoxinin. |
4(0,0,0,4) | Details |
| 11714703 | Zheng Y, Hirschberg B, Yuan J, Wang AP, Hunt DC, Ludmerer SW, Schmatz DM, Cully DF: Identification of two novel Drosophila melanogaster -gated chloride channel subunits expressed in the eye. J Biol Chem. 2002 Jan 18;277(3):2000-5. Epub 2001 Nov 19. -activated currents were not blocked by picrotoxinin, fipronil, strychnine, or the H2 antagonist cimetidine. |
3(0,0,0,3) | Details |
| 16027231 | Buckingham SD, Biggin PC, Sattelle BM, Brown LA, Sattelle DB: Insect GABA receptors: splicing, editing, and targeting by antiparasitics and insecticides. Mol Pharmacol. 2005 Oct;68(4):942-51. Epub 2005 Jul 18. A -gated chloride channel subunit from Drosophila melanogaster [Resistant to Dieldrin (RDL)] has been cloned, functionally expressed, and found to exhibit many aspects of the pharmacology of native, bicuculline-insensitive insect GABA receptors. RDL is the target of the commercially important insecticide fipronil. |
2(0,0,0,2) | Details |
| 12770091 | Le Corronc H, Alix P, Hue B: Differential sensitivity of two insect -gated channels to dieldrin, fipronil and picrotoxinin. J Insect Physiol. 2002 Apr;48(4):419-431. We describe here the pharmacological properties of two GABA receptor subtypes coupled to a chloride channel on dorsal unpaired median (DUM) neurones of the adult male cockroach. |
2(0,0,0,2) | Details |
| 19906878 | Dupuis JP, Bazelot M, Barbara GS, Paute S, Gauthier M, Raymond-Delpech V: Homomeric RDL and heteromeric RDL/LCCH3 GABA receptors in the honeybee antennal lobes: two candidates for inhibitory transmission in olfactory processing. J Neurophysiol. 2010 Jan;103(1):458-68. Epub 2009 Nov 11. -gated chloride channel receptors are abundant in the CNS, where their physiological role is to mediate fast inhibitory neurotransmission. The resulting receptors were activated by insect GABA-receptor agonists muscimol and CACA and blocked by antagonists fipronil, dieldrin, and picrotoxin, but not bicuculline, displaying a typical RDL-like pharmacology. |
2(0,0,0,2) | Details |
| 7885191 | Cole LM, Roush RT, Casida JE: Drosophila -gated chloride channel: modified [3H] EBOB binding site associated with --> Ser or Gly mutants of Rdl subunit. Life Sci. 1995;56(10):757-65. This specific binding of [3H] EBOB is strongly inhibited by: a large number and variety of insecticidal channel blockers at 20 nM (lindane, alpha-endosulfan, dieldrin, 12-ketoendrin, fipronil, and a representative bicycloorthobenzoate and dithiane) or 200 nM (picrotoxinin); the insecticidal channel activators avermectin and moxidectin at 20 nM; muscimol at 30 microM and GABA at 300 microM. |
2(0,0,0,2) | Details |
| 11879973 | Ratra GS, Erkkila BE, Weiss DS, Casida JE: Unique insecticide specificity of human homomeric rho 1 (C) receptor. . Toxicol Lett. 2002 Mar 24;129(1-2):47-53. Several convulsants and major insecticides block the -gated chloride channel in brain on binding to the (A) receptor. This (C) rho 1 receptor is very sensitive to CNBOB and lindane relative to alpha-endosulfan, tert-butylbicyclophosphorothionate, picrotoxinin and fipronil (IC (50) values of 23, 91, 800, 1080, 4000 and > 10000 nM, respectively, in displacing [3H] EBOB). |
2(0,0,0,2) | Details |
| 11312652 | Ratra GS, Kamita SG, Casida JE: Role of human (A) receptor beta3 subunit in insecticide toxicity. Toxicol Appl Pharmacol. 2001 May 1;172(3):233-40. The type A (A)) receptor is the target for the major insecticides alpha-endosulfan, lindane, and fipronil and for many analogs. Their action as chloride channel blockers is directly measured by binding studies with [(3) H] ethynylbicycloorthobenzoate ([(3) H] EBOB). |
1(0,0,0,1) | Details |
| 19336526 | McCavera S, Rogers AT, Yates DM, Woods DJ, Wolstenholme AJ: An ivermectin-sensitive -gated chloride channel from the parasitic nematode Haemonchus contortus. Mol Pharmacol. 2009 Jun;75(6):1347-55. Epub 2009 Mar 31. Responses to and ivermectin were inhibited by picrotoxinin and fipronil. |
1(0,0,0,1) | Details |
| 12590480 | Aajoud A, Ravanel P, Tissut M: Fipronil metabolism and dissipation in a simplified aquatic ecosystem. J Agric Food Chem. 2003 Feb 26;51(5):1347-52. Several phenylpyrazole derivatives are selective inhibitors of chloride channel activities in insects. |
1(0,0,0,1) | Details |
| 12442503 | Tingle CC, Rother JA, Dewhurst CF, Lauer S, King WJ: Fipronil: environmental fate, ecotoxicology, and human health concerns. Rev Environ Contam Toxicol. 2003;176:1-66. It belongs to the phenyl pyrazole or fiprole group of chemicals and is a potent disrupter of the insect central nervous system via interference with the -) regulated chloride channel. |
1(0,0,0,1) | Details |
| 10212398 | Wolff MA, Wingate VP: Characterization and comparative pharmacological studies of a functional (GABA) receptor cloned from the tobacco budworm, Heliothis virescens (Noctuidae:Lepidoptera). Invert Neurosci. 1998 Mar;3(4):305-15. Two electrode voltage clamp recordings of Xenopus oocytes expressing the HVRDL -gated chloride channel revealed robust ion conductance in response to and the GABAA receptor agonist, muscimol. conductance was depressed by the novel insecticide, fipronil ((+/-)-5-amino-1-(2,6 dichloro-alpha, alpha, alpha-trifluoro-p-tolyl)-4-trifluoromethyl-sulfinylpyrazole-3-carb onitrile) and the GABAA antagonist, picrotoxinin. |
1(0,0,0,1) | Details |
| 18651916 | Hirata K, Ishida C, Eguchi Y, Sakai K, Ozoe F, Ozoe Y, Matsuda K: Role of a serine residue (S278) in the pore-facing region of the housefly -gated chloride channel in determining sensitivity to noncompetitive antagonists. Insect Mol Biol. 2008 Aug;17(4):341-50. Gamma-hexachlorocyclohexane (gamma-HCH), fipronil and picrotoxinin are noncompetitive antagonists (NCAs) of -gated channels (GluCls), yet their potencies are weaker than those on gamma-aminobutyric acid receptors (GABARs). |
1(0,0,0,1) | Details |
| 20200125 | Janssen D, Derst C, Rigo JM, Van Kerkhove E: Cys-loop ligand-gated channels in Dorsal Unpaired Median neurons of Locusta migratoria. J Neurophysiol. 2010 Mar 3. In insects, inhibitory neurotransmission is generally associated with members of the cys-loop ligand-gated anion channels, such as the -gated chloride channel (GluCl), the gamma-amino -gated channels (GABACl) and the -gated channels (HisCl). GluCls were sensitive to ibotenate and blocked by picrotoxin and fipronil. |
1(0,0,0,1) | Details |
| 16537435 | Chen L, Durkin KA, Casida JE: Structural model for gamma-aminobutyric acid receptor noncompetitive antagonist binding: widely diverse structures fit the same site. Proc Natl Acad Sci U S A. 2006 Mar 28;103(13):5185-90. Epub 2006 Mar 10. Several major insecticides, including alpha-endosulfan, lindane, and fipronil, and the botanical picrotoxinin are noncompetitive antagonists (NCAs) for the GABA receptor. Despite large structural diversity, the NCAs are proposed to fit a single binding site in the chloride channel lumen lined by five transmembrane 2 segments. |
1(0,0,0,1) | Details |
| 11378196 | Cheeseman CL, Delany NS, Woods DJ, Wolstenholme AJ: High-affinity ivermectin binding to recombinant subunits of the Haemonchus contortus -gated chloride channel. Mol Biochem Parasitol. 2001 May;114(2):161-8. Picrotoxin, fipronil, and all failed to compete for ivermectin binding to either subunit. |
1(0,0,0,1) | Details |