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NEONICOTINOID INSECTICIDE TOXICOLOGY: Mechanisms of Selective Action
Abstract
▪ Abstract The neonicotinoids, the newest major class of insecticides, have outstanding potency and systemic action for crop protection against piercing-sucking pests, and they are highly effective for flea control on cats and dogs. Their common names are acetamiprid, clothianidin, dinotefuran, imidacloprid, nitenpyram, thiacloprid, and thiamethoxam. They generally have low toxicity to mammals (acute and chronic), birds, and fish. Biotransformations involve some activation reactions but largely detoxification mechanisms. In contrast to nicotine, epibatidine, and other ammonium or iminium nicotinoids, which are mostly protonated at physiological pH, the neonicotinoids are not protonated and have an electronegative nitro or cyano pharmacophore. Agonist recognition by the nicotinic receptor involves cation-π interaction for nicotinoids in mammals and possibly a cationic subsite for interaction with the nitro or cyano substituent of neonicotinoids in insects. The low affinity of neonicotinoids for vertebrate relative to insect nicotinic receptors is a major factor in their favorable toxicological profile.
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Cited by
Environmental fate and exposure; neonicotinoids and fipronil
Bonmatin, J.-M., Giorio, C., Girolami, V., Goulson, D., Kreutzweiser, D. P., Krupke, C., Liess, M., Long, E., Marzaro, M., Mitchell, E. A. D., et al. (2015) · Environmental Science and Pollution Research · doi:10.1007/s11356-014-3332-7 · Cited by 1,372
Declines in insectivorous birds are associated with high neonicotinoid concentrations
Hallmann, C. A., Foppen, R. P. B., van Turnhout, C. A. M., de Kroon, H., & Jongejans, E. (2014) · Nature · doi:10.1038/nature13531 · Cited by 1,052
Wildlife Ecotoxicology of Pesticides: Can We Track Effects to the Population Level and Beyond?
Köhler, H.-R., & Triebskorn, R. (2013) · Science · doi:10.1126/science.1237591 · Cited by 911
Chronic exposure to neonicotinoids reduces honey bee health near corn crops
Tsvetkov, N., Samson-Robert, O., Sood, K., Patel, H. S., Malena, D. A., Gajiwala, P. H., Maciukiewicz, P., Fournier, V., & Zayed, A. (2017) · Science · doi:10.1126/science.aam7470 · Cited by 555
Nkya, T. E., Akhouayri, I., Kisinza, W., & David, J.-P. (2013) · Insect Biochemistry and Molecular Biology · doi:10.1016/j.ibmb.2012.10.006 · Cited by 402
Metadata
- Authors
- Tomizawa, M., & Casida, J. E.
- Venue
- Annual Review of Pharmacology and Toxicology
- Publisher
- Annual Reviews
- Published
- 2005-09-22
- Volume
- 45
- Issue
- 1
- Pages
- 247-268
- ISSN
- 0362-1642 (ISSN-L)
- 1545-4304
- OpenAlex
- W2125205784
- Cited by
- 1,741
- References
- 0
- FWCI
- 1.38
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: NEONICOTINOID INSECTICIDE TOXICOLOGY: Mechanisms of Selective Action. https://app.cochat.ai/papers/10.1146/annurev.pharmtox.45.120403.095930
- The paper
- Tomizawa, M., & Casida, J. E. (2005). NEONICOTINOID INSECTICIDE TOXICOLOGY: Mechanisms of Selective Action. Annual Review of Pharmacology and Toxicology. https://doi.org/10.1146/annurev.pharmtox.45.120403.095930
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
