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Trends Pharmacol Sci. 2001 Nov;22(11):573-80.

Neonicotinoids: insecticides acting on insect nicotinic acetylcholine receptors.

Author information

1
Laboratory of Pesticide Chemistry, Dept of Agricultural Chemistry, Faculty of Agriculture, Kinki University, 3327-204 Nakamachi, 631-8505, Nara, Japan.

Abstract

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.

PMID:
11698101
DOI:
10.1016/s0165-6147(00)01820-4
[Indexed for MEDLINE]

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