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Journal ArticleDOI

Golden age of insecticide research: past, present, or future?

01 Jan 1998-Annual Review of Entomology (Annu Rev Entomol)-Vol. 43, Iss: 3, pp 1-16
TL;DR: Insecticide research, having passed through several Golden Ages, is now in a renaissance of integrating chemicals and biologicals for sustainable pest control with human safety.
Abstract: Insecticide research led to the first "complete" victories in combatting pests almost 50 years ago with the chlorinated hydrocarbons followed quickly by the organophosphates, methylcarbamates, and pyrethroids--all neuroactive chemicals. This Golden Age of Discovery was the source of most of our current insecticides. The challenge then became health and the environment, a Golden Age met with selective and degradable compounds. Next the focus shifted to resistance, novel biochemical targets, and new chemical approaches for pest control. The current Golden Age of Genetic Engineering has curtailed, but is unlikely to eliminate, chemical use on major crops. Insecticide research, having passed through several Golden Ages, is now in a renaissance of integrating chemicals and biologicals for sustainable pest control with human safety.
Citations
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Journal ArticleDOI
TL;DR: The neonicotinoids 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.
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 ...

1,409 citations


Cites background from "Golden age of insecticide research:..."

  • ...Pest insect control, an essential component of crop protection and public health, has evolved over a recorded history of three millennia (1, 2)....

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Journal ArticleDOI
TL;DR: The diverse toxic actions and pharmacological effects of pyrethroids suggest that simple additivity models based on combined actions at a single target are not appropriate to assess the risks of cumulative exposure to multiple pyre Throids.

849 citations


Cites background from "Golden age of insecticide research:..."

  • ...By the mid-1990s, pyrethroid use had grown to represent 23% of the U.S. dollar value of the world insecticide market, ranking second only to organophosphorus compounds among insecticide classes (Casida and Quistad, 1998)....

    [...]

  • ...Pyrethroids act in vitro on a variety of putative biochemical and physiological target sites, four of which merit consideration as sites of toxic action....

    [...]

Journal ArticleDOI
TL;DR: Knowledge reviewed here of the functional architecture and molecular aspects of the insect and mammalian nAChRs and their neonicotinoid-binding site lays the foundation for continued development and use of this new class of safe and effective insecticides.
Abstract: ■ Abstract Neonicotinoids, the most important new class of synthetic insecticides of the past three decades, are used to control sucking insects both on plants and on companion animals. Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). The botanical insecticide nicotine acts at the same target without the neonicotinoid level of effectiveness or safety. Fundamental differences between the nAChRs of insects and mammals confer remarkable selectivity for the neonicotinoids. Whereas ionized nicotine binds at an anionic subsite in the mammalian nAChR, the negatively tipped (“magic” nitro or cyano) neonicotinoids interact with a proposed unique subsite consisting of cationic amino acid residue(s) in the insect nAChR. Knowledge reviewed here of the functional architecture and molecular aspects of the insect and mammalian nAChRs and their neonicotinoid-binding site lays the foundation for continued development and use of this new class of safe and effective insecticides. CONTENTS

823 citations

Journal ArticleDOI
TL;DR: The phytochemical biomolecules could be used for maximizing the effectiveness and specificity in future insecticide design with specific or multiple target sites, while ensuring the economic and ecological sustainability.

641 citations

Journal ArticleDOI
TL;DR: Primary toxic effects in mammals from off-target serine hydrolase inhibition include organophosphate-induced delayed neuropathy and disruption of the cannabinoid system.
Abstract: Neuroactive insecticides are the principal means of protecting crops, people, livestock, and pets from pest insect attack and disease transmission. Currently, the four major nerve targets are acetylcholinesterase for organophosphates and methylcarbamates, the nicotinic acetylcholine receptor for neonicotinoids, the γ-aminobutyric acid receptor/chloride channel for polychlorocyclohexanes and fiproles, and the voltage-gated sodium channel for pyrethroids and dichlorodiphenyltrichloroethane. Species selectivity and acquired resistance are attributable in part to structural differences in binding subsites, receptor subunit interfaces, or transmembrane regions. Additional targets are sites in the sodium channel (indoxacarb and metaflumizone), the glutamate-gated chloride channel (avermectins), the octopamine receptor (amitraz metabolite), and the calcium-activated calcium channel (diamides). Secondary toxic effects in mammals from off-target serine hydrolase inhibition include organophosphate-induced delayed n...

633 citations

References
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Book ChapterDOI
01 Jan 1997
TL;DR: The use of synthetic organic insecticides has served for the past half century as the principal means to control insect-borne diseases and minimize losses in food and fibre production from pest insect attack as mentioned in this paper.
Abstract: Synthetic organic insecticides have served for the past half century as the principal means to control insect-borne diseases and minimize losses in food and fibre production from pest insect attack. Pests destroy about one-third of the world food supply during growth, harvesting and storage, even with the use of pesticides and other control methods (Ware, 1994). Without pesticides, especially in the tropics, there would be dramatic losses of crops, greatly exacerbating existing food shortages in developing countries (Forget, 1991). The world population is expected to grow by more than one billion people or about 20% in the next decade, which in turn also requires expanded use of agrochemicals for efficient agriculture. This can only be achieved by the most effective use of the current insecticides and the development of better compounds for the years ahead.

8 citations