HOUSE-FLY BRAIN GAMMA-AMINOBUTYRIC ACID-GATED CHLORIDE CHANNEL - TARGET FOR MULTIPLE CLASSES OF INSECTICIDES

被引:71
作者
DENG, YL [1 ]
PALMER, CJ [1 ]
CASIDA, JE [1 ]
机构
[1] UNIV CALIF BERKELEY,DEPT ENTOMOL SCI,PESTICIDE CHEM & TOXICOL LAB,BERKELEY,CA 94720
基金
美国国家卫生研究院;
关键词
D O I
10.1016/0048-3575(91)90060-Y
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The γ-aminobutyric acid receptor/chloride ionophore is the proposed target in insects for a wide range of commercial and candidate insecticides, a hypothesis that can be tested directly by developing a toxicologically relevant radioligand binding assay. This was achieved with house fly brain and 1-(4-ethynylphenyl)-4-[2,3-3H2]propyl-2,6,7-trioxabicyclo[2.2.2]octane ([3H]EBOB) for which the binding site was demonstrated to be identical to or overlapping with that of seven classes of structurally diverse insecticides, i.e., trioxabicyclooctanes, dithianes, silatranes, lindane, toxaphene, chlorinated cyclodienes, and picrotoxinin. The affinity of the binding site for this radioligand is reduced fourfold in a cyclodiene-resistant strain. There is no cross resistance to avermectin B1a and moxidectin which are potent noncompetitive inhibitors of [3H]EBOB binding. © 1991.
引用
收藏
页码:60 / 65
页数:6
相关论文
共 24 条
  • [1] ASATO G, 1988, Patent No. 259779
  • [2] BRADFORD MM, 1976, ANAL BIOCHEM, V72, P248, DOI 10.1016/0003-2697(76)90527-3
  • [3] CASIDA JE, 1985, MOL PHARMACOL, V28, P246
  • [4] CASIDA JE, 1988, NEUROTOX 88 MOL BASI, P125
  • [5] EFFECTS OF INSECTICIDES AND GABAERGIC AGENTS ON A HOUSEFLY [S-35] TERT-BUTYLBICYCLOPHOSPHOROTHIONATE BINDING-SITE
    COHEN, E
    CASIDA, JE
    [J]. PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY, 1986, 25 (01) : 63 - 72
  • [6] ELDEFRAWI ME, 1988, NEUROTOX 88 MOL BASI, P207
  • [7] ELLIOTT ME, 1990, 7TH INT C PEST CHEM
  • [8] FISHER MH, 1990, REC ADV CHEM INSECT, V2, P52
  • [9] 4-ALKYNYLPHENYLSILATRANES - INSECTICIDAL ACTIVITY, MAMMALIAN TOXICITY, AND MODE OF ACTION
    HORSHAM, MA
    PALMER, CJ
    COLE, LM
    CASIDA, JE
    [J]. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 1990, 38 (08) : 1734 - 1738
  • [10] INTERACTIONS OF LINDANE, TOXAPHENE AND CYCLODIENES WITH BRAIN-SPECIFIC TERT-BUTYLBICYCLOPHOSPHOROTHIONATE RECEPTOR
    LAWRENCE, LJ
    CASIDA, JE
    [J]. LIFE SCIENCES, 1984, 35 (02) : 171 - 178