Protein Information

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

Compound Information

Name dieldrin
CAS

Reference List

PubMed Abstract RScore(About this table)
8625394 Harrison JB, Chen HH, Sattelle E, Barker PJ, Huskisson NS, Rauh JJ, Bai D, Sattelle DB: Immunocytochemical mapping of a C-terminus anti-peptide antibody to the GABA receptor subunit, RDL in the nervous system in Drosophila melanogaster. Cell Tissue Res. 1996 May;284(2):269-78.

An antibody raised against a peptide based on the C-terminal derived amino acid sequence from a cloned Drosophila melanogaster (fruit fly) gene, Rdl (resistant to dieldrin), was used to investigate localization of a GABA receptor subunit in adult male D. melanogaster.
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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.

Resistance to cyclodiene insecticides is associated with replacements of a single amino acid (alanine 302) in a gamma-aminobutyric acid (GABA) receptor subunit encoded by the single-copy gene Resistance to dieldrin (Rdl).
8(0,0,1,3) Details
9372130 Aronstein K, Ffrench-Constant R: Immunocytochemistry of a novel GABA receptor subunit Rdl in Drosophila melanogaster. Invert Neurosci. 1995;1(1):25-31.

Following our recent cloning of a novel gamma-aminobutyric acid (GABA) receptor subunit gene Resistance to dieldrin or Rdl form cyclodiene resistance locus in Drosophila melanogaster, we were interested in defining its pattern of expression during development.
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8389005 Ffrench-Constant RH, Rocheleau TA, Steichen JC, Chalmers AE: A point mutation in a Drosophila GABA receptor confers insecticide resistance. Nature. 1993 Jun 3;363(6428):449-51.

Previously, we used a field-isolated Drosophila mutant Rdl (Resistant to dieldrin) insensitive to PTX and cyclodienes to clone a putative GABA receptor.
8(0,0,1,3) Details
7527461 Zhang HG, ffrench-Constant RH, Jackson MB: A unique amino acid of the Drosophila GABA receptor with influence on drug sensitivity by two mechanisms. J Physiol. 1994 Aug 15;479 ( Pt 1):65-75.

The Drosophila gene Rdl (resistance to dieldrin) encodes a GABA receptor.
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8601436 Shotkoski F, Zhang HG, Jackson MB, ffrench-Constant RH: Stable expression of insect GABA receptors in insect cell lines. FEBS Lett. 1996 Feb 19;380(3):257-62.

We are interested in establishing stably transformed insect cell lines efficiently expressing the insect gamma-aminobutyric acid (GABA) receptor subunit gene Resistance to dieldrin or Rdl.
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7704314 Shotkoski F, Lee HJ, Zhang HG, Jackson MB, ffrench-Constant RH: Functional expression of insecticide-resistant GABA receptors from the mosquito Aedes aegypti. Insect Mol Biol. 1994 Nov;3(4):283-7.

As a first step towards this goal, we here report the functional homomultimeric expression of a gamma-aminobutyric acid (GABA) receptor subunit gene, Resistance to dieldrin (Rdl), from the yellow fever mosquito Aedes aegypti in baculovirus-infected insect cell lines.
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7563084 Stilwell GE, Rocheleau T, ffrench-Constant RH: GABA receptor minigene rescues insecticide resistance phenotypes in Drosophila. J Mol Biol. 1995 Oct 20;253(2):223-7.

A single point mutation within the GABA receptor gene Resistance to dieldrin (Rdl) confers a high level of resistance to cyclodiene insecticides in a wide range of insects.
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9257933 Rauh JJ, Benner E, Schnee ME, Cordova D, Holyoke CW, Howard MH, Bai D, Buckingham SD, Hutton ML, Hamon A, Roush RT, Sattelle DB: Effects of [3H]-BIDN, a novel bicyclic dinitrile radioligand for GABA-gated chloride channels of insects and vertebrates. Br J Pharmacol. 1997 Aug;121(7):1496-505.

A variety of gamma-aminobutyric acid (GABA) receptor convulsants, including the insecticides heptachlor (IC50, 35 +/- 3 nM) and dieldrin (IC50, 93 +/- 7 nM), displaced [3H]-BIDN from rootworm membranes.
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17044880 Brooke BD, Hunt RH, Matambo TS, Koekemoer LL, Van Wyk P, Coetzee M: Dieldrin resistance in the malaria vector Anopheles gambiae in Ghana. Med Vet Entomol. 2006 Sep;20(3):294-9.

We conclude that dieldrin resistance in the An. gambiae population of the Obuasi region occurs at a high level - most likely in the absence of selection - and that control of the resistance phenotype is polyfactorial and must include components other than mutations in the GABA receptor locus.
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10761585 Ffrench-Constant RH, Anthony N, Aronstein K, Rocheleau T, Stilwell G: Cyclodiene insecticide resistance: from molecular to population genetics. Annu Rev Entomol. 2000;45:449-66.

Emphasis is given to the use of a resistant Drosophila mutant as an entry point to cloning the associated gamma-aminobutyric acid (GABA) receptor subunit gene, Resistance to dieldrin.
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9740020 Stilwell GE, ffrench-Constant RH: Transcriptional analysis of the Drosophila GABA receptor gene resistance to dieldrin. J Neurobiol. 1998 Sep 15;36(4):468-84.
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20188834 Tantely ML, Tortosa P, Alout H, Berticat C, Berthomieu A, Rutee A, Dehecq JS, Makoundou P, Labbe P, Pasteur N, Weill M: Insecticide resistance in Culex pipiens quinquefasciatus and Aedes albopictus mosquitoes from La Reunion Island. Insect Biochem Mol Biol. 2010 Feb 25.

A simple molecular test was developed to detect Rdl (R) allele, encoding a gamma-aminobutyric acid (GABA) receptor resistant to dieldrin.
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15796751 Du W, Awolola TS, Howell P, Koekemoer LL, Brooke BD, Benedict MQ, Coetzee M, Zheng L: Independent mutations in the Rdl locus confer dieldrin resistance to Anopheles gambiae and An. arabiensis. Insect Mol Biol. 2005 Apr;14(2):179-83.

Substitutions of a conserved alanine residue in the Rdl locus coding for a gamma-aminobutyric acid (GABA) receptor subunit with serine or glycine confer resistance to dieldrin in various insect species.
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9419893 Severson DW, Anthony NM, Andreev O, ffrench-Constant RH: Molecular mapping of insecticide resistance genes in the yellow fever mosquito (Aedes aegypti). J Hered. 1997 Nov-Dec;88(6):520-4.

The para sodium channel gene homologue and the GABA receptor gene Resistance to dieldrin map to the same genome regions as the DDT/pyrethroid and cyclodiene resistance loci, respectively.
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18093001 Narusuye K, Nakao T, Abe R, Nagatomi Y, Hirase K, Ozoe Y: Molecular cloning of a GABA receptor subunit from Laodelphax striatella (Fallen) and patch clamp analysis of the homo-oligomeric receptors expressed in a Drosophila cell line. Insect Mol Biol. 2007 Dec;16(6):723-33.

Antagonists such as fipronil (100 nM), 4'-ethynyl-4-n-propylbicycloorthobenzoate (EBOB) (100 nM), dieldrin (100 nM) and SR95531 (gabazine) (1 microM) suppressed GABA-induced currents.
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15578595 Bass C, Schroeder I, Turberg A, Field LM, Williamson MS: Identification of the Rdl mutation in laboratory and field strains of the cat flea, Ctenocephalides felis (Siphonaptera: Pulicidae). Pest Manag Sci. 2004 Dec;60(12):1157-62.

In many insect species, resistance to cyclodiene insecticides is caused by amino acid substitutions at a single residue (A302) within the M2 transmembrane region of the gamma-aminobutyric acid (GABA) receptor sub-unit termed Rdl (resistance to dieldrin).
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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-induced potentiation of current was observed only when the gamma 2 subunit was present in embryonic kidney cells (HEK-293) transfected with GABA receptor subunits.
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12642390 Bamber BA, Twyman RE, Jorgensen EM: Pharmacological characterization of the homomeric and heteromeric UNC-49 GABA receptors in C. elegans. Br J Pharmacol. 2003 Mar;138(5):883-93.

Picrotoxin sensitivity strongly correlates with dieldrin sensitivity, yet UNC-49B homomers were highly dieldrin resistant.
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7476913 Zhang HG, Lee HJ, Rocheleau T, ffrench-Constant RH, Jackson MB: Subunit composition determines picrotoxin and bicuculline sensitivity of Drosophila gamma-aminobutyric acid receptors. Mol Pharmacol. 1995 Nov;48(5):835-40.

These include Resistance to dieldrin, or Rdl, and a homologue of the vertebrate GABAA receptor beta subunit.
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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.
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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.

In the central nervous system of both vertebrates and invertebrates inhibitory neurotransmission is mainly achieved through activation of gamma-aminobutyric acid (GABA) receptors.
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1653332 Bermudez I, Hawkins CA, Taylor AM, Beadle DJ: Actions of insecticides on the insect GABA receptor complex. . J Recept Res. 1991;11(1-4):221-32.

In contrast dieldrin, ivermectin, lindane, picrotoxin and TBPS are inhibitors of [35S] TBPS binding at the nanomolar range.
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12766256 Zhao X, Salgado VL, Yeh JZ, Narahashi T: Differential actions of fipronil and dieldrin insecticides on GABA-gated chloride channels in cockroach neurons. J Pharmacol Exp Ther. 2003 Sep;306(3):914-24. Epub 2003 May 23.

Fipronil and dieldrin are known to inhibit GABA receptors in both mammals and insects.
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10952672 Grolleau F, Sattelle DB: Single channel analysis of the blocking actions of BIDN and fipronil on a Drosophila melanogaster GABA receptor (RDL) stably expressed in a Drosophila cell line. Br J Pharmacol. 2000 Aug;130(8):1833-42.

Single channel recordings were obtained from a DROSOPHILA: S2 cell line stably expressing the wild-type RDL (ac) Drosophila melanogaster homomer-forming ionotropic GABA receptor subunit, a product of the resistance to dieldrin gene, RDL: GABA (50 microM) was applied by pressure ejection to outside-out patches from S2-RDL cells at a holding potential of -60 mV.
83(1,1,1,3) Details
9014156 Buckingham SD, Matsuda K, Hosie AM, Baylis HA, Squire MD, Lansdell SJ, Millar NS, Sattelle B: Wild-type and insecticide-resistant homo-oligomeric GABA receptors of Drosophila melanogaster stably expressed in a Drosophila cell line. Neuropharmacology. 1996;35(9-10):1393-401.

Here, we report the generation of a Drosophila melanogaster cell line (S2-RDLA302S) stably expressing a mutated, dieldrin-resistant (A302S) form of RDL.
2(0,0,0,2) Details
16758255 Hosie AM, Buckingham SD, Hamon A, Sattelle DB: Replacement of asparagine with arginine at the extracellular end of the second transmembrane (M2) region of insect GABA receptors increases sensitivity to penicillin G. Invert Neurosci. 2006 Jun;6(2):75-9. Epub 2006 Apr 29.

The A301S mutation that confers resistance to dieldrin did not significantly affect the antagonism by PCG.
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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.
It seems that general anesthetics have a specific affinity for the GABA receptor-channel complex.
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3000377 Bloomquist JR, Soderlund DM: Neurotoxic insecticides inhibit GABA-dependent chloride uptake by mouse brain vesicles. Biochem Biophys Res Commun. 1985 Nov 27;133(1):37-43.

The neurotoxic insecticides endrin, dieldrin, aldrin, lindane (gamma-1,2,3,4,5,6-hexachlorocyclohexane) and deltamethrin inhibited gamma-aminobutyric acid-dependent 36Cl- uptake by mouse brain vesicles.
These results demonstrate the disruption of gamma-aminobutyric acid receptor-chloride ionophore function in mammalian brain by neurotoxic insecticides and provide evidence that this complex is the principal site of cyclodiene action.
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12370061 Narahashi T: Nerve membrane ion channels as the target site of insecticides. Mini Rev Med Chem. 2002 Aug;2(4):419-32.

Dieldrin, lindane and fipronil block GABA receptors.
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1593011 Smyth KA, Parker AG, Yen JL, McKenzie JA: Selection of dieldrin-resistant strains of Lucilia cuprina (Diptera: Calliphoridae) after ethyl methanesulfonate mutagenesis of a susceptible strain. J Econ Entomol. 1992 Apr;85(2):352-8.

Dieldrin resistance may be caused by less effective blocking of insect neuronal GABA receptors by the chemical in resistant strains.
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9087552 Thompson M, Steichen JC, ffrench-Constant RH: Conservation of cyclodiene insecticide resistance-associated mutations in insects. Insect Mol Biol. 1993;2(3):149-54.


In Drosophila melanogaster resistance is associated with a single base pair substitution in the GABA receptor/chloride ion channel gene Rdl.
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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.

Endosulfan resistance was associated with a moderate level of resistance to dieldrin, and resistance to both insecticides was due, in part, to increased detoxification by glutathione S-transferases (GST).
The endosulfan resistant strain displayed the same amino acid at position 302 of the Rdl gene (GABA receptor) as susceptible aphids (e.g.
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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.
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 Ala--> Ser or Gly replacement.
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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.
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1311215 Bloomquist JR, Roush RT, ffrench-Constant RH: Reduced neuronal sensitivity to dieldrin and picrotoxinin in a cyclodiene-resistant strain of Drosophila melanogaster (Meigen). Arch Insect Biochem Physiol. 1992;19(1):17-25.

The possible role of an altered GABA receptor in this resistance is discussed.
1(0,0,0,1) Details
9831449 Ikeda T, Nagata K, Shono T, Narahashi T: Dieldrin and picrotoxinin modulation of GABA (A) receptor single channels. Neuroreport. 1998 Oct 5;9(14):3189-95.

Previous studies have demonstrated that dieldrin and picrotoxin share the common binding site on the GABA receptor.
81(1,1,1,1) 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.

The HVRDL GABA receptor was insensitive to blockage by dieldrin and the GABAA antagonist, bicuculline.
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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.

Mutant RDL GABA-receptors, which have a naturally occurring amino acid substitution (A302--> S) in the putative ion-channel lining region, conferring resistance to dieldrin and picrotoxinin, were markedly less sensitive to fipronil than the wild-type receptors. 4.
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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.

Gamma-hexachlorocyclohexane (gamma-HCH), fipronil and picrotoxinin are noncompetitive antagonists (NCAs) of L-glutamate-gated chloride channels (GluCls), yet their potencies are weaker than those on gamma-aminobutyric acid receptors (GABARs).
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.
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3009836 Abalis IM, Eldefrawi ME, Eldefrawi AT: Effects of insecticides on GABA-induced chloride 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 gamma-aminobutyric acid (GABA) receptors were studied on the function of GABAA receptors in rat brain as assayed by GABA-induced 36Cl- influx into membrane microsacs.
The GABA-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.
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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 gamma-aminobutyric acid (GABA) receptor gene from P. xylostella, PxRdl, were cloned and sequenced.
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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.

The subunit gene encoded a 483-amino acid polypeptide that showed 84% sequence identity with DmRdl subunit (U02042) (Drosophila melanogaster resistant to dieldrin).
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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.
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8982503 Hosie AM, Ozoe Y, Koike K, Ohmoto T, Nikaido T, Sattelle DB: Actions of picrodendrin antagonists on dieldrin-sensitive and -resistant Drosophila GABA receptors. Br J Pharmacol. 1996 Dec;119(8):1569-76.
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18520997 Es-Salah Z, Lapied B, Le Goff G, Hamon A: RNA editing regulates insect gamma-aminobutyric acid receptor function and insecticide sensitivity. Neuroreport. 2008 Jun 11;19(9):939-43.

In Drosophila, the resistance to dieldrin (RDL) gamma-aminobutyric acid (GABA) receptor subunit displays an editing site (R122) that is close to the putative GABA-binding site.
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12510900 Andreasen MH, Ffrench-Constant RH: In situ hybridization to the Rdl locus on polytene chromosome 3L of Anopheles stephensi. Med Vet Entomol. 2002 Dec;16(4):452-5.

We are interested in generating a Y-autosome translocation of the Resistance to dieldrin (Rdl) locus in the malaria vector mosquito Anopheles stephensi Liston (Diptera: Culicidae), for use in sterile insect release.
These fragments encode the second membrane-spanning region of the gamma-aminobutyric acid receptor and show high levels of both nucleotide and predicted amino acid identity to other Rdl-like receptors.
1(0,0,0,1) Details
8653417 Hosie AM, Shirai Y, Buckingham SD, Rauh JJ, Roush RT, Baylis HA, Sattelle DB: Blocking actions of BIDN, a bicyclic dinitrile convulsant compound, on wild-type and dieldrin-resistant GABA receptor homo-oligomers of Drosophila melanogaster expressed in Xenopus oocytes. Brain Res. 1995 Sep 25;693(1-2):257-60.
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10198127 Andreev D, Kreitman M, Phillips TW, Beeman RW, ffrench-Constant RH: Multiple origins of cyclodiene insecticide resistance in Tribolium castaneum (Coleoptera: Tenebrionidae). J Mol Evol. 1999 May;48(5):615-24.

Target-site insensitivity to cyclodienes is conferred by single point mutations in the gene Resistance to dieldrin (Rdl), which codes for a subunit of a gamma-aminobutyric acid (GABA) receptor.
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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.
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1651498 Ffrench-Constant RH, Mortlock DP, Shaffer CD, MacIntyre RJ, Roush RT: Molecular cloning and transformation of cyclodiene resistance in Drosophila: an invertebrate gamma-aminobutyric acid subtype A receptor locus. Proc Natl Acad Sci U S A. 1991 Aug 15;88(16):7209-13.


To our knowledge, this represents the first cloning of an invertebrate GABA receptor and also allows us to manipulate the resistance status of an insect via germ-line transformation.
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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.

Dieldrin stimulation requires the gamma2s subunit in the GABA receptor, whereas dieldrin suppression occurs in the presence or absence of the gamma2s subunit.
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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.
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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.
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7603613 Shirai Y, Hosie AM, Buckingham SD, Holyoke CW Jr, Baylis HA, Sattelle DB: Actions of picrotoxinin analogues on an expressed, homo-oligomeric GABA receptor of Drosophila melanogaster. Neurosci Lett. 1995 Apr 7;189(1):1-4.

The actions of picrotoxinin and four of its analogues were tested on a Drosophila melanogaster homo-oligomeric GABA (gamma-aminobutyric acid) receptor formed when RDL (resistance to dieldrin) subunits were expressed in Xenopus oocytes.
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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.

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15148245 Gisselmann G, Plonka J, Pusch H, Hatt H: Drosophila melanogaster GRD and LCCH3 subunits form heteromultimeric GABA-gated cation channels. Br J Pharmacol. 2004 Jun;142(3):409-13. Epub 2004 May 17.


Picrotoxin effectively blocked the GABA-gated channel (IC50=0.25 microm), but bicuculline, TPMTA, dieldrin and lindane did not.
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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.
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20180551 McGonigle I, Lummis SC: Molecular characterization of agonists that bind to an insect GABA receptor. Biochemistry. 2010 Apr 6;49(13):2897-902.

One of the most widely studied insect GABA receptors is constructed from RDL (resistance to dieldrin) subunits from Drosophila melanogaster.
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10679793 Hollins B, McClintock TS: Lobster GABA receptor subunit expressed in neural tissues. J Neurosci Res. 2000 Feb 15;59(4):534-41.

The sequences were most similar to the Drosophila RDL (resistance to dieldrin) GABA subunit with 54% identity, and 30-35% identity with vertebrate ionotropic GABA receptor subunits.
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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.
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