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      Discovery, research and development of axalion® active insecticide: dimpropyridaz

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      Pest Management Science
      Wiley

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          Abstract

          Dimpropyridaz is a novel insecticide active ingredient (a.i.) for the control of piercing and sucking pests. The discovery of dimpropyridaz included the synthesis of thousands of compound analogs which were investigated for their potential efficacy and registrability. Dimpropyridaz is the sole representative of the pyridazine pyrazolecarboxamide class, Insecticide Resistance Action Committee ( IRAC) Group 36. The novel mode of action is characterized by disrupting the function of an insect's chordotonal organs in a way that is distinctly different from IRAC Groups 9 and 29. Dimpropyridaz demonstrates translaminar and systemic effects as well as high selectivity, providing both application flexibility and, when applied according to the label, beneficial organism, and environmental compatibility. Dimpropyridaz, powered formulations will be available in select markets, covering a broad range of vegetable, fruit, row crop, and ornamental production segments. Dimpropyridaz also has commercial registered name: Axalion Active. This review will focus on a broad outline of the chemical preparation, regulatory overview, and select biological performance and represents a summary of the information shared during the invited lecture at the 15th IUPAC (International Union of Pure and Applied Chemistry) International Congress of Crop Protection Chemistry held in New Delhi, India in March 2023. © 2024 BASF. Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

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          Chordotonal Organs of Insects

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            TRP Channels in Insect Stretch Receptors as Insecticide Targets.

            Defining the molecular targets of insecticides is crucial for assessing their selectivity and potential impact on environment and health. Two commercial insecticides are now shown to target a transient receptor potential (TRP) ion channel complex that is unique to insect stretch receptor cells. Pymetrozine and pyrifluquinazon disturbed Drosophila coordination and hearing by acting on chordotonal stretch receptor neurons. This action required the two TRPs Nanchung (Nan) and Inactive (Iav), which co-occur exclusively within these cells. Nan and Iav together sufficed to confer cellular insecticide responses in vivo and in vitro, and the two insecticides were identified as specific agonists of Nan-Iav complexes that, by promoting cellular calcium influx, silence the stretch receptor cells. This establishes TRPs as insecticide targets and defines specific agonists of insect TRPs. It also shows that TRPs can render insecticides cell-type selective and puts forward TRP targets to reduce side effects on non-target species.
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              Afidopyropen: New and potent modulator of insect transient receptor potential channels.

              The commercial insecticides pymetrozine and pyrifluquinazon control plant-sucking pests by disturbing their coordination and ability to feed. We have previously shown that these compounds act by overstimulating and eventually silencing vanilloid-type transient receptor potential (TRPV) channels, which consist of two proteins, Nanchung and Inactive, that are co-expressed exclusively in insect chordotonal stretch receptor neurons. Here we show that a new insecticidal compound, afidopyropen, modulates chordotonal organs of American grasshoppers (Schistocerca americana) in the same fashion. Afidopyropen stimulated heterologously expressed TRPV channels from two different insect species - fruit fly (Drosophila melanogaster) and pea aphid (Acyrthosiphon pisum) - but did not affect function of the mammalian TRPV channel TRPV4. Activation of the insect TRPVs required simultaneous expression of both Nanchung and Inactive proteins. Tritium-labeled afidopyropen bound fruit fly TRPVs with higher affinity than pymetrozine and competed with pymetrozine for binding. Nanchung protein formed the main binding interface for afidopyropen, whereas co-expression of Inactive dramatically increased binding affinity. Another modulator of chordotonal organs, flonicamid, did not activate insect TRPV channels, nor did it compete with afidopyropen for binding, indicating that it has a different target site. These results define afidopyropen as a new, potent and specific modulator of insect TRPV channels, and provide insight into the unique binding mode of these compounds.
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                Author and article information

                Contributors
                (View ORCID Profile)
                Journal
                Pest Management Science
                Pest Management Science
                Wiley
                1526-498X
                1526-4998
                September 25 2024
                Affiliations
                [1 ] Global Insecticides Research and Development ‐ Agronomy BASF Corporation Research Triangle Park NC USA
                Article
                10.1002/ps.8385
                97179eee-0ecf-4339-bd6f-2f514f8b989b
                © 2024

                http://creativecommons.org/licenses/by-nc-nd/4.0/

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