Modes of Action, Resistance and Toxicity of Insecticides Targeting Nicotinic Acetylcholine Receptors

Author(s): Makoto Ihara, Steven D. Buckingham, Kazuhiko Matsuda, David B. Sattelle*

Journal Name: Current Medicinal Chemistry

Volume 24 , Issue 27 , 2017

  Journal Home
Translate in Chinese
Become EABM
Become Reviewer
Call for Editor


Background: Nicotinic acetylcholine receptors (nAChRs) of insects play a key role in fast excitatory neurotransmission. Several classes of insecticides target insect nAChRs, which are composed of subunit members of a family of multiple subunit encoding genes. Alternative splicing and RNA A-to-I editing can add further to receptor diversity. Native and recombinant receptors have been explored as sites of insecticide action using radioligands, electrophysiology and site-directed mutagenesis.

Methods: We have reviewed the properties of native and recombinant insect nAChRs, the challenges of functional recombinant insect nAChR expression, nAChR interactions with ligands acting at orthosteric and allosteric sites and in particular their interactions with insecticides.

Results: Actions on insect nAChRs of cartap, neonicotinoids, spinosyns, sulfoxamines, butenolides and mesoionic insecticides are reviewed and current knowledge of their modes of action are addressed. Mutations that add to our understanding of insecticide action and those leading to resistance are discussed. Co-crystallisation of neonicotinoids with the acetylcholine binding protein (AChBP), a surrogate for the nAChR ligand binding domain, has proved instructive. Toxicity issues relating to insecticides targeting nAChRs are also considered.

Conclusion: An overview of insecticide classes targeting insect nAChRs has enhanced our understanding of these important receptors and their insecticide binding sites. However, the subunit composition of native nAChRs remains poorly understood and functional expression still presents difficulties. These topics together with improved understanding of the precise sites of insecticide actions on insect nAChRs will be the subject of future research.

Keywords: Nicotinic acetylcholine receptor, neonicotinoids, spinosyns, sulfoximines, butenolides, triflumezopyrim, insecticide, resistance, toxicity.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2017
Published on: 21 September, 2017
Page: [2925 - 2934]
Pages: 10
DOI: 10.2174/0929867324666170206142019
Price: $65

Article Metrics

PDF: 85
PRC: 1