Protein Information

Name chloride channel (protein family or complex)
Synonyms chloride channel

Compound Information

Name dieldrin
CAS

Reference List

PubMed Abstract RScore(About this table)
8597060 Narahashi T, Carter DB, Frey J, Ginsburg K, Hamilton BJ, Nagata K, Roy ML, Song JH, Tatebayashi H: Sodium channels and GABAA receptor-channel complex as targets of environmental toxicants. Toxicol Lett. 1995 Dec;82-83:239-45.

Dieldrin had a dual action on the GABAA receptor-chloride channel complex of rat dorsal root ganglion neurons.
82(1,1,1,2) Details
6204183 Lawrence LJ, Casida JE: Interactions of lindane, toxaphene and cyclodienes with brain-specific t-butylbicyclophosphorothionate receptor. Life Sci. 1984 Jul 9;35(2):171-8.

Three major classes of chlorinated hydrocarbon insecticides, i.e., the lindane/hexachlorocyclohexane, toxaphene and aldrin/dieldrin types, are potent, competitive, and stereospecific inhibitors of t-butylbicyclophosphorothionate (TBPS) binding to brain-specific sites, thereby indicating an action at the gamma-aminobutyric acid (GABA)-regulated chloride channel.
81(1,1,1,1) 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 GABA responses recorded from Xenopus oocytes expressing either wild type (dieldrin-sensitive) or mutant (dieldrin-resistant) forms of the Drosophila melanogaster GABA-gated chloride channel homo-oligomer, RDL (the product of the resistance to dieldrin locus: Rdl). 2.
81(1,1,1,1) Details
8062082 Nagata K, Hamilton BJ, Carter DB, Narahashi T: Selective effects of dieldrin on the GABAA receptor-channel subunits expressed in human embryonic kidney cells. Brain Res. 1994 May 9;645(1-2):19-26.

We have recently demonstrated that the cyclodiene insecticide dieldrin modulates the kinetics of the GABAA receptor-chloride channel complex of rat dorsal root ganglion neurons in a complex manner, causing both stimulatory and inhibitory effects.
81(1,1,1,1) Details
9745915 Narahashi T, Ginsburg KS, Nagata K, Song JH, Tatebayashi H: Ion channels as targets for insecticides. Neurotoxicology. 1998 Aug-Oct;19(4-5):581-90.

The major site of action of dieldrin and hexachlorocyclohexane is the GABA (A) receptor chloride channel complex.
81(1,1,1,1) Details
8169820 Nagata K, Narahashi T: Dual action of the cyclodiene insecticide dieldrin on the gamma-aminobutyric acid receptor-chloride channel complex of rat dorsal root ganglion neurons. J Pharmacol Exp Ther. 1994 Apr;269(1):164-71.
62(0,2,2,2) Details
12770577 Zheng Y, Priest B, Cully DF, Ludmerer SW: RdlDv, a novel GABA-gated chloride channel gene from the American dog tick Dermacentor variabilis. Insect Biochem Mol Biol. 2003 Jun;33(6):595-9.

The closest homologue of the predicted gene product of RdlDv is the RDL protein encoded by the GABA-gated chloride channel gene Drosophila Rdl (Resistance to Dieldrin), with which it shares 64% amino acid identity.
34(0,1,1,4) Details
12770091 Le Corronc H, Alix P, Hue B: Differential sensitivity of two insect GABA-gated chloride channels to dieldrin, fipronil and picrotoxinin. J Insect Physiol. 2002 Apr;48(4):419-431.

Exposure to dieldrin decreases only the early phase of the muscimol and CACA-induced biphasic response, suggesting that two GABA-gated chloride channel receptor subtypes are present in DUM neurones.
32(0,1,1,2) 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.

Molecular analysis of the GABA-responding cells revealed that both subunits RDL and LCCH3 were expressed out of the three orthologs of Drosophila melanogaster GABA-receptor subunits encoded within the honeybee genome (RDL, resistant to dieldrin; GRD, GABA/glycine-like receptor of Drosophila; LCCH3, ligand-gated chloride channel homologue 3), opening the door to possible homo- and/or heteromeric associations.
32(0,1,1,2) Details
10455279 Matsuda K, Hosie AM, Holyoke CW Jr, Rauh JJ, Sattelle DB: Cross-resistance with dieldrin of a novel tricyclic dinitrile GABA receptor antagonist. Br J Pharmacol. 1999 Jul;127(6):1305-7.

A novel tricyclic dinitrile, KN244, blocked the wild-type (dieldrin-sensitive) homo-oligomeric gamma-aminobutyric acid (GABA)-gated chloride channel of Drosophila melanogaster expressed in Xenopus oocytes.
31(0,1,1,1) 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 GABA-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.
7(0,0,1,2) Details
8054658 Bloomquist JR: Cyclodiene resistance at the insect GABA receptor/chloride channel complex confers broad cross resistance to convulsants and experimental phenylpyrazole insecticides. Arch Insect Biochem Physiol. 1994;26(1):69-79.

The Maryland strain of D. melanogaster was resistant to dieldrin, lindane, picrotoxinin, TBPS, p-CN-TBOB, and JKU 0422.
3(0,0,0,3) Details
7885191 Cole LM, Roush RT, Casida JE: Drosophila GABA-gated chloride channel: modified [3H] EBOB binding site associated with Ala--> 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
10725394 Hold KM, Sirisoma NS, Ikeda T, Narahashi T, Casida JE: Alpha-thujone (the active component of absinthe): gamma-aminobutyric acid type A receptor modulation and metabolic detoxification. Proc Natl Acad Sci U S A. 2000 Apr 11;97(8):3826-31.


Second, a strain of Drosophila specifically resistant to chloride channel blockers is also tolerant to alpha-thujone.
2(0,0,0,2) Details
10212398 Wolff MA, Wingate VP: Characterization and comparative pharmacological studies of a functional gamma-aminobutyric acid (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 GABA-gated chloride channel revealed robust chloride ion conductance in response to GABA and the GABAA receptor agonist, muscimol.
The HVRDL GABA receptor was insensitive to blockage by dieldrin and the GABAA antagonist, bicuculline.
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 L-glutamate-gated chloride channel in determining sensitivity to noncompetitive antagonists. Insect Mol Biol. 2008 Aug;17(4):341-50.

The A302S mutation of Drosophila RDL (resistant to dieldrin) GABAR confers NCA resistance, and housefly GluCls (MdGluCls) possess S278 as the residue corresponding to the A302.
1(0,0,0,1) Details
1722072 Narahashi T: Transmitter-activated ion channels as the target of chemical agents. Adv Exp Med Biol. 1991;287:61-73.

Lindane and the cyclodienes dieldrin, endrin, heptachlor-epoxide, and isobenzan suppressed the GABA-activated chloride current.
The GABA-activated chloride channel has been shown to be modulated by general anesthetics, alcohols, and the pyrethroid, cyclodiene and lindane insecticides.
1(0,0,0,1) Details
14637375 Ikeda T, Zhao X, Kono Y, Yeh JZ, Narahashi T: Fipronil modulation of glutamate-induced chloride currents in cockroach thoracic ganglion neurons. Neurotoxicology. 2003 Dec;24(6):807-15.

Although fipronil is known to block GABA receptors, the mechanisms of its selective toxicity and efficacy against insects with dieldrin-resistant GABA receptors are not fully understood.
We studied the effects of fipronil on the inhibitory glutamate receptor-chloride channel complex, which is found only in invertebrates.
1(0,0,0,1) Details
19133471 Zhou XM, Wu QJ, Zhang YJ, Bai LY, Huang XY: Cloning and characterization of a GABA receptor from Plutella xylostella (Lepidoptera: Plutellidae). J Econ Entomol. 2008 Dec;101(6):1888-96.

A full-length cDNA, with an open reading frame (ORF) of 1,449 bp, encoding a subunit of the gamma-aminobutyric acid (GABA)-activated chloride channel was isolated from Plutella xylostella (L.) (Lepidoptera: Plutellidae) (GenBank accession no.
The subunit gene encoded a 483-amino acid polypeptide that showed 84% sequence identity with DmRdl subunit (U02042) (Drosophila melanogaster resistant to dieldrin).
1(0,0,0,1) Details
2409983 Abalis IM, Eldefrawi ME, Eldefrawi AT: Binding of GABA receptor channel drugs to a putative voltage-dependent chloride channel in Torpedo electric organ. Biochem Pharmacol. 1985 Jul 15;34(14):2579-82.

1(0,0,0,1) Details
2556203 Holden-Dye L, Krogsgaard-Larsen P, Nielsen L, Walker RJ: GABA receptors on the somatic muscle cells of the parasitic nematode, Ascaris suum: stereoselectivity indicates similarity to a GABAA-type agonist recognition site. Br J Pharmacol. 1989 Nov;98(3):841-50.


The Ascaris GABA receptor does not recognise agents that are known to block the GABA gated chloride channel in mammalian preparations such as t-butylbicyclophosphorothionate (TBPS, 10 microM, n = 2) or the insecticide dieldrin (100 microM, n = 3). 7.
0(0,0,0,0) Details
1663556 Payne GT, Soderlund DM: Activation of gamma-aminobutyric acid insensitive chloride channels in mouse brain synaptic vesicles by avermectin B1a. J Biochem Toxicol. 1991 Winter;6(4):283-92.


However, the chlorinated cycloalkane insecticides dieldrin and lindane were equally effective as inhibitors of GABA-dependent chloride uptake and AVMB1a-stimulated chloride efflux.
0(0,0,0,0) Details