| Name | GABA receptor (protein family or complex) |
|---|---|
| Synonyms | GABA receptor; GABA receptors; GABA(A) receptor; GABA(A) receptors; Gamma aminobutyric acid receptor; Gamma aminobutyric acid receptors |
| Name | alpha-endosulfan |
|---|---|
| CAS | (3α,5aβ,6α,9α,9aβ)-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) | |
|---|---|---|---|
| 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. |
83(1,1,1,3) | Details |
| 6090849 | Cole LM, Lawrence LJ, Casida JE: Similar properties of [35S] t-butylbicyclophosphorothionate receptor and coupled components of the GABA receptor-ionophore complex in brains of human, cow, rat, chicken and fish. Life Sci. 1984 Oct 22;35(17):1755-62. As a possible exception, chicken and fish brain membranes appear to be less sensitive than the others to the insecticide alpha-endosulfan. |
3(0,0,0,3) | Details |
| 11489356 | Ratra GS, Casida JE: GABA receptor subunit composition relative to insecticide potency and selectivity. Toxicol Lett. 2001 Jul 6;122(3):215-22. First, from published data, alpha-endosulfan, lindane and fipronil compete for the [(3) H] EBOB binding site with affinities of 0.3--7 nM in both human recombinant homooligomeric beta 3 receptors and housefly head membranes. |
3(0,0,0,3) | 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. |
3(0,0,0,3) | Details |
| 18446586 | Law RJ, Lightstone FC: Gaba receptor insecticide non-competitive antagonists may bind at allosteric modulator sites. Int J Neurosci. 2008 May;118(5):705-34. Results from several studies have shown that a series of chemically distinct insecticide compounds (picrotoxin, BIDN, TBPS, fipronil, lindane, EBOB, and alpha-endosulfan) affect A receptor function. |
2(0,0,0,2) | 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. The GABA receptor was prepared by ultra centrifugation and dialysis of brain homogenates of either cow, goat, rat or catfish. A radioreceptor assay protocol was developed to measure the amount of the alpha-endosulfan in blood samples. |
1(0,0,0,1) | 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. [3H] Ethynylbicycloorthobenzoate ([3H] EBOB) is a recently developed specific radioligand for the noncompetitive blocker site of the (GABA) receptor, which is the target of many polychlorocycloalkane and heterocyclic insecticides. -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). |
1(0,0,0,1) | 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. Cyclodiene resistance in D. melanogaster has been attributed to a mutation resulting in an Ala302--> Ser replacement in the Rdl GABA receptor subunit and in D. simulans to an homologous --> Ser or Gly replacement. |
1(0,0,0,1) | Details |