Neonicotinoid Insecticides: Molecular Targets, Resistance, and Toxicity

Neonicotinoids have been used to protect crops and animals from insect pests since the 1990s, but there are concerns regarding their adverse effects on nontarget organisms, notably on bees. Enhanced resistance to neonicotinoids in pests is becoming well documented. We address the current understanding of neonicotinoid target site interactions, selectivity, and metabolism not only in pests but also in beneficial insects such as bees. The findings are relevant to the management of both neonicotinoids and the new generation of pesticides targeting insect nicotinic acetylcholine receptors.

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A hypothesis to account for the selective and diverse actions of neonicotinoid insecticides at their molecular targets, nicotinic acetylcholine receptors: catch and release in hydrogen bond networks

Invertebrate Neuroscience ◽

10.1007/s10158-006-0043-x ◽

2007 ◽

Vol 7 (1) ◽

pp. 47-51 ◽

Cited By ~ 20

Author(s):

Makoto Ihara ◽

Masaru Shimomura ◽

Chiharu Ishida ◽

Hisashi Nishiwaki ◽

Miki Akamatsu ◽

...

Keyword(s):

Hydrogen Bond ◽

Nicotinic Acetylcholine Receptors ◽

Acetylcholine Receptors ◽

Molecular Targets ◽

Nicotinic Acetylcholine ◽

Neonicotinoid Insecticides ◽

Catch And Release ◽

Hydrogen Bond Networks

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Importance of nicotinic acetylcholine receptors in the visual adverse effects associated with telithromycin

Biochemical Pharmacology ◽

10.1016/j.bcp.2009.06.087 ◽

2009 ◽

Vol 78 (7) ◽

pp. 922

Author(s):

D. Bertrand ◽

S. Bertrand ◽

P. Fernandes

Keyword(s):

Adverse Effects ◽

Nicotinic Acetylcholine Receptors ◽

Acetylcholine Receptors ◽

Nicotinic Acetylcholine

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Neonicotinoids disrupt memory, circadian behaviour and sleep

10.1101/2020.04.07.030171 ◽

2020 ◽

Cited By ~ 1

Author(s):

Kiah Tasman ◽

Sergio Hidalgo ◽

Edgar Buhl ◽

Sean A. Rands ◽

James J.L. Hodge

Keyword(s):

Acetylcholine Receptor ◽

Nicotinic Acetylcholine Receptor ◽

Nicotinic Acetylcholine Receptors ◽

Acetylcholine Receptors ◽

Circadian Rhythmicity ◽

Insect Brain ◽

Nicotinic Acetylcholine ◽

Pigment Dispersing Factor ◽

Beneficial Insects ◽

Pollinating Insects

SummaryGlobally, neonicotinoids are still the most used insecticides, despite their well-documented sub-lethal effects on beneficial insects1. Neonicotinoids are agonists at the nicotinic acetylcholine receptors, the main mediator of synaptic transmission in the insect brain2–5, making them highly potent neurotoxins and insecticides6,7. Memory, circadian rhythmicity and sleep are essential for efficient foraging in many pollinating insects, and involve nicotinic acetylcholine receptor signalling2,4,8–10. The effect of field-relevant concentrations of European Union-banned neonicotinoids: imidacloprid, clothianidin and thiamethoxam, as well as the currently unbanned thiacloprid were tested on Drosophila memory, circadian rhythms and sleep. Field-relevant concentrations of imidacloprid, clothianidin and thiamethoxam disrupted learning, behavioural rhythmicity and sleep whilst thiacloprid exposure only affected sleep. Exposure to imidacloprid and clothianidin directly affected neurophysiology, preventing the day/night remodelling and accumulation of pigment dispersing factor neuropeptide in the dorsal terminals of clock neurons. Knockdown of the neonicotinoid susceptible Dα1 and Dβ2 nicotinic acetylcholine receptor subunits in the mushroom bodies or clock neurons recapitulated the neonicotinoid like deficits in memory or circadian/sleep behaviour demonstrating that neonicotinoid effects are likely mediated in the mushroom body and clock circuitry. Disruption to learning, circadian rhythmicity and sleep are likely to have far-reaching detrimental effects on beneficial insects in the field.

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Molecular Characterization of Off-Target Activities of Telithromycin: a Potential Role for Nicotinic Acetylcholine Receptors

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00840-10 ◽

2010 ◽

Vol 54 (12) ◽

pp. 5399-5402 ◽

Cited By ~ 51

Author(s):

Daniel Bertrand ◽

Sonia Bertrand ◽

Estelle Neveu ◽

Prabhavathi Fernandes

Keyword(s):

Side Effects ◽

Adverse Effects ◽

Nicotinic Acetylcholine Receptors ◽

Acetylcholine Receptors ◽

Potential Role ◽

Visual Disturbance ◽

Ciliary Ganglion ◽

Clinical Use ◽

Nicotinic Acetylcholine

ABSTRACT Adverse effects have limited the clinical use of telithromycin. Preferential inhibition of the nicotinic acetylcholine receptors (nAChR) at the neuromuscular junction (α3β2 and NMJ), the ciliary ganglion of the eye (α3β4 and α7), and the vagus nerve innervating the liver (α7) could account for the exacerbation of myasthenia gravis, the visual disturbance, and the liver failure seen with telithromycin use. The studies presented here enable the prediction of expected side effects of macrolides in development, such as solithromycin (CEM-101).

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