Dinotefuran is an orally active and competitive inhibitor and insecticide targeting insect nicotinic acetylcholine receptors ( nAChRs ). Dinotefuran blocks neural signaling and induces neural dysfunction in insects. Dinotefuran binds to [ 3 H]epibatidine in the neural cord membrane of American cockroach with an IC 50 of 890 nM and to [ 3 H]α-bungarotoxin with an IC 50 of 36.1 μM. Dinotefuran exhibits knockdown activity (KD 50 =0.351 nmol/g) and lethal activity (LD 50 =0.173 nmol/g) against German cockroach. Dinotefuran is mainly used for agricultural pest control, such as field control of piercing-sucking and chewing insects (e.g., aphids, planthoppers), while its environmental toxicological effects (e.g., oxidative stress and reproductive neurotoxicity on earthworms) are also a research focus to assess ecological risks.
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