| 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 | 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) | |
|---|---|---|---|
| 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 |
| 10333576 | Rufingier C, Pasteur N, Lagnel J, Martin C, Navajas M: Mechanisms of insecticide resistance in the aphid Nasonovia ribisnigri (Mosley) (Homoptera: Aphididae) from France. Insect Biochem Mol Biol. 1999 Apr;29(4):385-91. The endosulfan resistant strain displayed the same amino acid at position 302 of the Rdl gene (GABA receptor) as susceptible aphids (e.g. |
6(0,0,1,1) | 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 |
| 9862468 | Anthony N, Unruh T, Ganser D, ffrench-Constant R: Duplication of the Rdl GABA receptor subunit gene in an insecticide-resistant aphid, Myzus persicae. Mol Gen Genet. 1998 Nov;260(2-3):165-75. |
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 |
| 7568233 | Brun LO, Stuart J, Gaudichon V, Aronstein K, French-Constant RH: Functional haplodiploidy: a mechanism for the spread of insecticide resistance in an important international insect pest. Proc Natl Acad Sci U S A. 1995 Oct 10;92(21):9861-5. We investigated the genetics associated with this interesting life history after the important discovery of resistance to the cyclodiene type insecticide endosulfan. Both the inheritance of the resistance phenotype and the resistance-associated point mutation in the gamma-aminobutyric acid receptor gene Rdl were examined. |
1(0,0,0,1) | Details |
| 3009836 | Abalis IM, Eldefrawi ME, Eldefrawi AT: Effects of insecticides on -induced influx into rat brain microsacs. J Toxicol Environ Health. 1986;18(1):13-23. The actions of different insecticides known to affect binding of ligands to (GABA) receptors were studied on the function of GABAA receptors in rat brain as assayed by -induced 36Cl- influx into membrane microsacs. The -induced 36Cl- flux was inhibited by several cyclodienes and gamma-hexachlorocyclohexane (gamma-BHC) with the following order of decreasing potency: endosulfan I greater than endrin greater than endosulfan II greater than dieldrin greater than heptachlor epoxide greater than gamma-BHC greater than heptachlor. |
1(0,0,0,1) | 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 |
| 16813330 | Li A, Yang Y, Wu S, Li C, Wu Y: Investigation of resistance mechanisms to fipronil in diamondback moth (Lepidoptera: Plutellidae). J Econ Entomol. 2006 Jun;99(3):914-9. The selection resulted in 300-fold increase in resistance to fipronil, and 3.5- and 6.5-fold cross-resistance to dieldrin and endosulfan, respectively, in the SZ-F strain compared with the unselected SZ strain. The genomic DNA fragments flanking the second membrane-spanning region of Rdl (GABA) receptor gene from P. xylostella, PxRdl, were cloned and sequenced. |
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 |
| 2458634 | Matsumoto K, Eldefrawi ME, Eldefrawi AT: Action of polychlorocycloalkane insecticides on binding of [35S] t-butylbicyclophosphorothionate to Torpedo electric organ membranes and stereospecificity of the binding site. Toxicol Appl Pharmacol. 1988 Sep 15;95(2):220-9. Endrin was more potent than dieldrin, but endosulfan I and II had similar effects. |
0(0,0,0,0) | Details |