Neonicotinoids: insecticides acting on insect nicotinic acetylcholine receptors

被引：742

作者：

Matsuda, K

Buckingham, SD

Kleier, D

Rauh, JJ

Grauso, M

Sattelle, DB

机构：

[1] Kinki Univ, Fac Agr, Dept Agr Chem, Lab Pesticide Chem, Nara 6318505, Japan

[2] Univ Cambridge, Dept Zool, Babraham Inst, Mol Signalling Lab, Cambridge CB2 3EJ, England

[3] Dupont Agr Prod, Stine Haskell Res Ctr, Newark, DE 19714 USA

[4] Univ Oxford, Dept Human Anat & Genet, MRC, Funct Genet Unit, Oxford OX1 3QX, England

来源：

TRENDS IN PHARMACOLOGICAL SCIENCES | 2001年 / 22卷 / 11期

关键词：

D O I：

10.1016/S0165-6147(00)01820-4

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Imidacloprid is increasingly used worldwide as an insecticide. It is an agonist at nicotinic acetylcholine receptors (nAChRs) and shows selective toxicity for insects over vertebrates. Recent studies using binding assays, molecular biology and electrophysiology suggest that both alpha- and non-alpha -subunits of nAChRs contribute to interactions of these receptors with imidacloprid. Electrostatic interactions of the nitroimine group and bridgehead nitrogen in imidacloprid with particular nAChR amino acid residues are likely to have key roles in determining the selective toxicity of imidacloprid. Chemical calculation of atomic charges of the insecticide molecule and a site-directed mutagenesis study support this hypothesis.

引用

页码：573 / 580

页数：8

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