Neonicotinoids insect nAChR agonists

Table 29.1.4 Comparison between electro-physiological and [ H]-7 displacement potencies for different neonicotinoids 6-9, 13 and ( )-epibatidin (16) on insect nAChRs. Electrophysiological data [ECso and relative (agonist) efficacy] were obtained from neuron cell bodies isolated from the CNS of H. virescens. EC50 and relative efficacy values represent the mean of separate experiments on different neurons. Inhibition of [ H]-7 binding to nAChR in housefly head membrane preparations by the compounds is expressed as piso (piso values (= -log M) correspond to the concentration of cold ligand displacing 50% of bound [ H]-7 from housefly head membranes).

Neonicotinoid insecticides act agonistically on insect nicotinic acetylcholine receptors (nAChRs). Like imidacloprid (IMI), all neonicotinoids bind with high affinity (Iso-values 1 nM) to binding sites on... 

Neonicotinoids are insecticides acting on insect nAChRs (1). For a long time they are very effective on commercially important Hemipteran pest species such as aphids, whiteflies and planthoppers, but also control Coleopteran and some Lepidopteran pests (/). The biochemical mode of action (MoA) of neonicotinoids has been studied and characterized extensively in the past 10 years. Ail neonicotinoids act selectively as agonists at the insect nAChRs and they are part of a single MoA group as defmed by the Insecticide Resistance Action Committee (IRAC an Expert Conunittee of Crop Life) for resistance management purposes (2). Today the neonicotinoids are ... 

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