| Name | chloride channel (protein family or complex) |
|---|---|
| Synonyms | chloride channel |
| Name | endosulfan |
|---|---|
| CAS | 6,7,8,9,10,10-hexachloro-1,5,5a,6,9,9a-hexahydro-6,9-methano-2,4,3-benzodioxathiepin 3-oxide |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 7679302 | Casida JE: Insecticide action at the -gated chloride channel: recognition, progress, and prospects. Arch Insect Biochem Physiol. 1993;22(1-2):13-23. Three billion (3 x 10 (9)) pounds of hexachlorocyclohexanes, polychlorobornanes, and chlorinated cyclodienes (such as lindane, toxaphene, and endosulfan, respectively) were used to control pest insects before their mode of action was established as blocking the -gated chloride channel. |
82(1,1,1,2) | 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 |
| 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 |
| 8968340 | Huang J, Casida JE: Characterization of [3H] ethynylbicycloorthobenzoate ([3H] EBOB) binding and the action of insecticides on the -gated chloride channel in cultured cerebellar granule neurons. J Pharmacol Exp Ther. 1996 Dec;279(3):1191-6. -stimulated 36Cl- influx is also inhibited by seven insecticidal compounds (including EBOB, 12-ketoendrin and alpha-endosulfan) as well as picrotoxinin and t-butylbicyclophosphorothionate with IC50 levels ranging from 290 to 15300 nM, which correlate well (r = 0.92) with their inhibitory potencies for [3H] EBOB binding (1 to 773 nM). |
3(0,0,0,3) | Details |
| 8270763 | Saleh MA, Abou Zied M, el-Baroty G, Abdel-Reheim E, Abdel-Rahman F, Wallace C, el-Sebae AH, Blancato JN: radioreceptor-assay a possible biomarker for human exposure to certain agrochemicals. J Environ Sci Health B. 1993 Dec;28(6):687-99. Cyclodiene insecticides, hexachlorocyclohexanes, pyrethroids, bicyclophosphates, the bicycloorthocarboxylate insecticides and some of their metabolites and environmental degradation products are central nervous system toxicants with high specific binding affinity to the chloride channel of the A receptor-ionophore sites. [35S] tertiary-butylbicyclophosphorothionate (TBPS) with specific activity higher than 60 Ci/mmole has a high binding affinity to the same sites and is now commercially available and can be used to label the GABAA receptor for the development of a radioreceptor assay technique. A radioreceptor assay protocol was developed to measure the amount of the alpha-endosulfan in blood samples. |
1(0,0,0,1) | 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 |
| 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 |
| 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 |
| 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 |
| 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. The first generation includes the polychlorocycloalkanes alpha-endosulfan and lindane. |
1(0,0,0,1) | Details |
| 9147380 | Huang J, Casida JE: Role of cerebellar granule cell-specific GABAA receptor subtype in the differential sensitivity of [3H] ethynylbicycloorthobenzoate binding to mimetics. Neurosci Lett. 1997 Apr 4;225(2):85-8. In contrast, the inhibitory potencies of two chloride channel blockers, alpha-endosulfan and picrotoxinin, do not differ in these assays. |
0(0,0,0,0) | Details |