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Titolo:
GABA receptor subunit composition relative to insecticide potency and selectivity
Autore:
Ratra, GS; Casida, JE;
Indirizzi:
Univ Calif Berkeley, Dept Environm Sci Policy & Management, Environm Chem & Toxicol Lab, Berkeley, CA 94720 USA Univ Calif Berkeley Berkeley CA USA 94720 col Lab, Berkeley, CA 94720 USA
Titolo Testata:
TOXICOLOGY LETTERS
fascicolo: 3, volume: 122, anno: 2001,
pagine: 215 - 222
SICI:
0378-4274(20010706)122:3<215:GRSCRT>2.0.ZU;2-M
Fonte:
ISI
Lingua:
ENG
Soggetto:
GATED CHLORIDE CHANNEL; BINDING-SITES; FUNCTIONAL EXPRESSION; FIPRONIL INSECTICIDE; BRAIN; PHARMACOLOGY; RECOGNITION; SUBTYPES; HEAD;
Keywords:
gamma-aminobutryic acid; binding site specificity; [H-3]EBOB; alpha-endosulfan; fipronil; GABA receptor; GABA receptor subunits; insecticide; lindane; subunit composition;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
29
Recensione:
Indirizzi per estratti:
Indirizzo: Casida, JE Univ Calif Berkeley, Dept Environm Sci Policy & Management, Environm Chem & Toxicol Lab, 115 Wellman Hall, Berkeley, CA 94720 USA Univ Calif Berkeley 115 Wellman Hall Berkeley CA USA 94720 USA
Citazione:
G.S. Ratra e J.E. Casida, "GABA receptor subunit composition relative to insecticide potency and selectivity", TOX LETT, 122(3), 2001, pp. 215-222

Abstract

Three observations on the 4-[H-3]propyl-4 ' -ethynylbicycloorthobenzoate ([H-3]EBOB) binding site in the gamma -aminobutyric acid (GABA) receptor indicate the specific target for insecticide action in human brain and a possible mechanism for selectivity. First, from published data, alpha -endosulfan, lindane and fipronil compete for the [H-3]EBOB binding site with affinities of 0.3-7 nM in both human recombinant homooligomeric beta3 receptors and housefly head membranes. Second, from structure-activity studies, including new data, GABAergic insecticide binding potency on the pentameric receptor formed from the beta3 subunit correlates well with that on the housefly receptor (r = 0.88, n = 20). This conserved inhibitor specificity is consistent with known sequence homologies in the housefly GABA receptor and the human GABA(A) receptor beta3 subunit. Third, as mostly new findings, variouscombinations of alpha1, alpha6, and gamma2 subunits coexpressed with a beta1 or beta3 subunit confer differential insecticide binding sensitivity, particularly to fipronil, indicating that subunit composition is a major factor in insecticide selectivity. (C) 2001 Elsevier Science Ireland Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/09/20 alle ore 12:38:35