Selective actions of insecticides on desensitizing and non‐desensitizing nicotinic acetylcholine receptors in cockroach (<scp><i>Periplaneta americana</i></scp>) neurons

Salgado, Vincent L.

doi:10.1002/ps.6396

Cited by 13 publications

(9 citation statements)

References 33 publications

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“…Electrophysiological studies with native tissues or recombinant receptors showed that low concentrations of neonicotinoids can block nAChR, while higher concentrations can activate the receptor [ 7 , 24 ]. Therefore, it is still unclear whether insecticidal activity is the consequence of nAChR inhibition or activation in vivo.…”

Section: Discussionmentioning

confidence: 99%

Nicotinic acetylcholine receptor modulator insecticides act on diverse receptor subtypes with distinct subunit compositions

Liu

Fan

et al. 2022

PLoS Genet

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Insect nicotinic acetylcholine receptors (nAChRs) are pentameric ligand-gated ion channels mainly expressed in the central nervous system of insects. They are the directed targets of many insecticides, including neonicotinoids, which are the most widely used insecticides in the world. However, the development of resistance in pests and the negative impacts on bee pollinators affect the application of insecticides and have created a demand for alternatives. Thus, it is very important to understand the mode of action of these insecticides, which is not fully understood at the molecular level. In this study, we systematically examined the susceptibility of ten Drosophila melanogaster nAChR subunit mutants to eleven insecticides acting on nAChRs. Our results showed that there are several subtypes of nAChRs with distinct subunit compositions that are responsible for the toxicity of different insecticides. At least three of them are the major molecular targets of seven structurally similar neonicotinoids in vivo. Moreover, spinosyns may act exclusively on the α6 homomeric pentamers but not any other nAChRs. Behavioral assays using thermogenetic tools further confirmed the bioassay results and supported the idea that receptor activation rather than inhibition leads to the insecticidal effects of neonicotinoids. The present findings reveal native nAChR subunit interactions with various insecticides and have important implications for the management of resistance and the development of novel insecticides targeting these important ion channels.

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Section: Discussionmentioning

confidence: 99%

Nicotinic acetylcholine receptor modulator insecticides act on diverse receptor subtypes with distinct subunit compositions

Liu

Fan

et al. 2022

PLoS Genet

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show abstract

“…Electrophysiological studies with native tissues or recombinant receptors showed that low concentrations of neonicotinoids can block nAChR while higher concentrations cause receptor activation [7,23]. Therefore, it is still unclear whether the insecticidal activity is the consequence of nAChR inhibition or activation in vivo.…”

Section: Discussionmentioning

confidence: 99%

Nicotinic modulation insecticides act on diverse receptor subtypes with distinct subunit compositions

Liu

Fan

et al. 2021

Preprint

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Insect nicotinic acetylcholine receptors (nAChRs) are ligand gated ion channels mainly expressed in the central nervous system of insects. They are the directed targets of nicotinic modulation insecticides including neonicotinoids, the most widely used insecticides in the world. However, the resistance development from pests and the negative impacts on the pollinators affect their applications and create demand for the alternatives. Thus, it is very important to understand the mode of action of these insecticides at the molecular level, which is actually unclear for more than 30 years. In this study, we systematically examined the susceptibility of ten Drosophila melanogaster nAChR subunits mutants against eleven nicotinic modulation insecticides. Our results showed that there are several subtypes of nAChRs with distinct subunits compositions that are responsible for the toxicity of different insecticides, respectively. At least three of them are the major molecular targets of seven structurally similar neonicotinoids in vivo. On the other hand, the spinosyns may exclusively act on the α6 homomeric nAChR but not any other heteromeric pentamers. Behavioral assays using thermogenetic tools further confirmed the bioassay results and support the idea that receptor activation rather than inhibition leads to the insecticidal effects of neonicotinoids. The present findings reveal native nAChR subunit interactions with various insecticides and have important implications for resistance management and the development of novel insecticides targeting this important ion channels.Author SummaryThe neonicotinoids and spinosyns make up about 27% of the insecticides by world market value. Novel insecticides like sulfoxaflor, flupyradifurone and triflumezopyrim are developed as alternatives due to the negative effects of neonicotinoids on pollinators. Although all act via insect nicotinic acetylcholine receptors, the mode of action is unclear. Our work shows that these insecticides act on diverse receptor subtypes with distinct subunit compositions. This finding could lead to the development of more selective insecticides to control pests with minimal effects on beneficial insects.

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“…Vincent Salgado gave his award address on nAChRs, an area which he further advances in his research paper detailing the differences between desensitizing and non‐desensitizing nAChRs 7 . He has studied this target for many years while at several different industrial research facilities.…”

Section: Research Articlesmentioning

confidence: 99%

Understanding the biological action of insecticides is the key to their continuous improvement

David¹,

Leibowitz²,

Lorsbach

et al. 2021

Pest Management Science

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Selective actions of insecticides on desensitizing and non‐desensitizing nicotinic acetylcholine receptors in cockroach (Periplaneta americana) neurons

Cited by 13 publications

References 33 publications

Nicotinic acetylcholine receptor modulator insecticides act on diverse receptor subtypes with distinct subunit compositions

Nicotinic acetylcholine receptor modulator insecticides act on diverse receptor subtypes with distinct subunit compositions

Nicotinic modulation insecticides act on diverse receptor subtypes with distinct subunit compositions

Understanding the biological action of insecticides is the key to their continuous improvement

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