Radiolabeled anthranilic diamide insecticide [N-C(3)H(3)]chlorantraniliprole was synthesized at high specific activity. It was compared with phthalic diamide insecticide flubendiamide and [(3)H]ryanodine in radioligand binding studies with house fly muscle membranes to provide the first direct evidence with a native insect ryanodine receptor that the major anthranilic and phthalic diamide insecticides bind at different allosterically coupled sites, i.e., there are three distinct Ca(2+)-release channel targets for insecticide action.
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http://dx.doi.org/10.1021/tx300326m | DOI Listing |
J Agric Food Chem
November 2024
College of Plant Protection, State & Local Joint Engineering Research Center of Green Pesticide Invention and Application, Nanjing Agricultural University, Weigang Road 1, Nanjing, Jiangsu 210095, China.
Chemosphere
November 2024
Bayer AG, Crop Science Division, R&D, 40789, Monheim, Germany. Electronic address:
Pestic Biochem Physiol
November 2024
Laboratoire Physiologie, Ecologie et Environnement (P2E), USC-INRAE 1328, Université d'Orléans, 1 rue de Chartres, 45067 Orléans, France; Institut Universitaire de France, 1 rue Descartes, 75005 Paris, France. Electronic address:
Insect neuronal nicotinic acetylcholine receptors (nAChRs) are transmembrane receptors that play a key role in the development and synaptic plasticity of both vertebrates and invertebrates, and are considered to be major targets of several insecticides. We used dorsal unpaired median (DUM) neurons, which are insect neurosecretory cells, to explore what type of nAChRs are involved in flupyradifurone's (FLU) mode of action, and to study the role of calcium release from intracellular stores in this process. Using whole-cell patch-clamp and fura-2-AM calcium imaging techniques, we found that inhibition of IPRs through application of 2-APB reduced FLU inward currents, but did not affect the intracellular calcium release induced by FLU.
View Article and Find Full Text PDFNat Commun
October 2024
Tianjin Key Laboratory for Modern Drug Delivery and High-Efficiency, Frontiers Science Center for Synthetic Biology, School of Pharmaceutical Science and Technology, Faculty of Medicine, Tianjin University, Tianjin, China.
J Agric Food Chem
October 2024
State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals of Guizhou University, Guiyang 550025, China.
Chlorantraniliprole (CHL), a favored agricultural insecticide, is renowned for its high efficiency and broad-spectrum effectiveness against lepidoptera insects. However, the urgency for new insecticide development is underscored by the intricate multistep preparation process and modest overall yields of CHL, along with the escalating challenge of insect resistance. In response, we have crafted CHL mimics from proline employing computer-aided drug design.
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