| Name | gamma aminobutyric acid 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 | lindane |
|---|---|
| CAS | (1α,2α,3β,4α,5α,6β)-1,2,3,4,5,6-hexachlorocyclohexane |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 9530529 | Anand M, Agrawal AK, Rehmani BN, Gupta GS, Rana MD, Seth PK: Role of GABA receptor complex in low dose lindane (HCH) induced neurotoxicity: neurobehavioural, neurochemical and electrophysiological studies. Drug Chem Toxicol. 1998 Feb;21(1):35-46. |
81(1,1,1,1) | Details |
| 9590437 | Vale C, Damgaard I, Sunol C, Rodriguez-Farre E, Schousboe A: Cytotoxic action of lindane in cerebellar granule neurons is mediated by interaction with inducible GABA (B) receptors. J Neurosci Res. 1998 May 1;52(3):286-94. However, in THIP-treated cultures, lindane-induced cytotoxicity was found to be mediated by an action of the insecticide on GABA receptors. |
81(1,1,1,1) | Details |
| 1377327 | Woodward RM, Polenzani L, Miledi R: Effects of hexachlorocyclohexanes on gamma-aminobutyric acid receptors expressed in Xenopus oocytes by RNA from mammalian brain and retina. Mol Pharmacol. 1992 Jun;41(6):1107-15. The pharmacology of the bicuculline/baclofen-insensitive GABA receptors was further investigated by comparing actions of hexachlorocyclohexane (HCH) enantiomers on -activated membrane currents expressed in oocytes by brain and retina RNA. gamma-HCH (lindane) was a potent inhibitor of IG-Actx, with suppression of currents detectable at concentrations as low as 50 nM. |
32(0,1,1,2) | Details |
| 11279263 | Katoh-Semba R, Takeuchi IK, Inaguma Y, Ichisaka S, Hata Y, Tsumoto T, Iwai M, Mikoshiba K, Kato K: Induction of brain-derived neurotrophic factor by convulsant drugs in the rat brain: involvement of region-specific voltage-dependent channels. J Neurochem. 2001 Apr;77(1):71-83. To elucidate possible mechanisms of endogenous BDNF increase, changes in levels of BDNF were studied in the rat brain following systemic administration of various convulsant agents; excitotoxic agonists, kainic acid and (+/-)-alpha-amino-3--5-methylisoxazole-4- (AMPA); GABA receptor antagonists, picrotoxin, pentylenetetrazole (PTZ) and lindane (gamma-hexachlorocyclohexane); and L-type voltage-dependent calcium channel agonist, BAY-K 8644. |
31(0,1,1,1) | Details |
| 12770368 | Aydar E, Beadle DJ: The pharmacological profile of GABA receptors on cultured insect neurones. J Insect Physiol. 1999 Mar;45(3):213-219. The receptors were modulated by the enantiomers of lindane. |
4(0,0,0,4) | 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 |
| 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. responses in neurons from the mutant strains showed reduced sensitivity to the antagonists picrotoxin, lindane and t-butyl-bicyclophosphorothionate. |
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 |
| 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. |
2(0,0,0,2) | Details |
| 1722072 | Narahashi T: Transmitter-activated ion channels as the target of chemical agents. Adv Exp Med Biol. 1991;287:61-73. The -activated chloride channel has been shown to be modulated by general anesthetics, and the pyrethroid, cyclodiene and lindane insecticides. It seems that general anesthetics have a specific affinity for the GABA receptor-channel complex. |
2(0,0,0,2) | 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 |
| 10401548 | Belelli D, Pau D, Cabras G, Peters JA, Lambert JJ: A single amino acid confers barbiturate sensitivity upon the rho 1 receptor. Br J Pharmacol. 1999 Jun;127(3):601-4. By contrast, GABA receptors composed of the rho 1 subunit are anaesthetic-insensitive. |
1(0,0,0,1) | Details |
| 8949935 | Nagata K, Huang CS, Hamilton BJ, Carter DB, Narahashi T: Differential effects of hexachlorocyclohexane isomers on the GABA receptor subunits expressed in human embryonic kidney cell line. Brain Res. 1996 Oct 28;738(1):131-7. |
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 -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 -gated channels (GluCls), yet their potencies are weaker than those on gamma-aminobutyric acid receptors (GABARs). |
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 |
| 7534833 | Pomes A, Frandsen A, Sunol C, Sanfeliu C, Rodriguez-Farre E, Schousboe A: Lindane cytotoxicity in cultured neocortical neurons is ameliorated by and flunitrazepam. J Neurosci Res. 1994 Dec 15;39(6):663-8. It is concluded that the cytotoxic action of lindane is mediated through interaction with GABA receptors in a manner essentially independent of changes in intracellular Ca2+ homeostasis. |
112(1,2,2,2) | 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. |
83(1,1,1,3) | Details |
| 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. |
82(1,1,1,2) | Details |
| 10397639 | Vale C, Vilaro MT, Rodriguez-Farre E, Sunol C: Effects of the conformationally restricted analogues, cis- and trans-4-aminocrotonic acid, on neurotransmission in primary neuronal cultures. J Neurosci Res. 1999 Jul 1;57(1):95-105. Both isomers induced a Cl- influx, which was inhibited by bicuculline, t-butylbicyclophosphorothionate (TBPS), picrotoxinin (PTX), and gamma-hexachlorocyclohexane (gamma-HCH or lindane). [3H]-flunitrazepam binding was also increased by both isomers and this increase was inhibited by bicuculline. The results presented here show that p-1 subunits, and thus GABAc receptors, may represent a very minor population of GABA receptors in these neuronal preparations. |
1(0,0,0,1) | 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. |
1(0,0,0,1) | 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. The gamma-aminobutyric acidA (GABAA) receptor-chloride channel complex is known to be the target site of dieldrin, a cyclodiene insecticide, and lindane. |
1(0,0,0,1) | Details |
| 7535710 | Feigenspan A, Bormann J: Differential pharmacology of GABAA and GABAC receptors on rat retinal bipolar cells. Eur J Pharmacol. 1994 Dec 15;288(1):97-104. These results demonstrate that rod bipolar cells possess two populations of pharmacologically distinct GABA receptors, GABAA and novel-type GABAC receptors, which might subserve different physiological functions in controlling visual transduction in the retina. |
1(0,0,0,1) | Details |
| 8750965 | Nagata K, Narahashi T: Differential effects of hexachlorocyclohexane isomers on the GABA receptor-chloride channel complex in rat dorsal root ganglion neurons. Brain Res. 1995 Dec 15;704(1):85-91. |
1(0,0,0,1) | Details |
| 1371151 | Vendrell M, Tusell JM, Serratosa J: c-fos expression as a model for studying the action of hexachlorocyclohexane isomers in the CNS. J Neurochem. 1992 Mar;58(3):862-9. The organochlorine insecticide gamma-hexachlorocyclohexane (gamma-HCH, lindane) has been shown to induce c-fos expression in different brain areas. Pentylenetetrazole and picrotoxin, a known gamma-aminobutyric acid-receptor antagonist, have also been considered. |
1(0,0,0,1) | Details |
| 9032455 | Silvestroni L, Fiorini R, Palleschi S: Partition of the organochlorine insecticide lindane into the human sperm surface induces membrane depolarization and Ca2+ influx. Biochem J. 1997 Feb 1;321 ( Pt 3):691-8. |
0(0,0,0,0) | Details |
| 15148245 | Gisselmann G, Plonka J, Pusch H, Hatt H: Drosophila melanogaster GRD and LCCH3 subunits form heteromultimeric -gated cation channels. Br J Pharmacol. 2004 Jun;142(3):409-13. Epub 2004 May 17. Picrotoxin effectively blocked the -gated channel (IC50=0.25 microm), but bicuculline, TPMTA, dieldrin and lindane did not. |
0(0,0,0,0) | Details |