Resistance to insecticides and acaricides is a major impediment to effectively controlling insect pests worldwide. These pests include the two-spotted spider mite Tetranychus urticae (T. urticae), which exists globally. This polyphagous herbivore causes major agricultural problems and can develop resistance to the agents above. Therefore, the continuous development of acaricides with new modes of action is important to circumvent the resistance of insects to pesticides. Acynonapyr is a novel class of acaricides containing an azabicyclo ring. In this study, we determined the activity of acynonapyr and its analogs on calcium-activated potassium (K2) channels in two-spotted spider mites using electrophysiological techniques (patch-clamp). We also examined their acaricidal efficacy against mites in the laboratory. The acynonapyr and analogs blocked T. urticae K2 (TurK2) channels in a concentration-dependent manner. A comparison of acaricidal activity against T. urticae with inhibitory activity against TurK2 revealed that TurK2 channels are the primary toxicological targets. Finally, we examined the effect of acynonapyr on Homo sapiens K2 (HsaK2.2) channels and demonstrated that the compound at 10 μM had a limited effect on the activity of this channel.
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http://dx.doi.org/10.1016/j.pestbp.2024.106074 | DOI Listing |
Cells
January 2025
Department of Chemistry, Biology and Biotechnologies, University of Perugia, Via dell'Elce di Sotto 8, 06123 Perugia, Italy.
Cells
December 2024
Department of Biology and Biochemistry, University of Houston, Houston, TX 77204, USA.
Podocytes express large-conductance Ca-activated K channels (BK channels) and at least two different pore-forming KCa1.1 subunit C-terminal splice variants, known as VEDEC and EMVYR, along with auxiliary β and γ subunits. Podocyte KCa1.
View Article and Find Full Text PDFJ Alzheimers Dis
January 2025
Division of Cardiothoracic Surgery, Rhode Island Hospital, Alpert Medical School of Brown University, Providence, RI, USA.
Proc Natl Acad Sci U S A
January 2025
Instituto de Neurociencias, Centro Interdisciplinario de Neurociencia de Valparaíso, Facultad de Ciencias, Universidad de Valparaíso, Valparaíso 2340000, Chile.
BK channels can control neuronal function, but their functional relevance in activity-dependent changes of synaptic function remains elusive. Here, we report that repetitive low-frequency stimulation activates BK channels through 12(S)HPETE, an arachidonic acid metabolite, produced downstream of postsynaptic metabotropic glutamate receptors (mGluRs) to trigger long-term depression (LTD) at CA3-CA1 synapses in hippocampal slices from P7-P10 mice. Activation of BK channels is subunit specific, as paxilline but not iberiotoxin blocked mGluR-LTD.
View Article and Find Full Text PDFMol Ther
January 2025
Institute for Chemical Research, Kyoto University, Uji, Kyoto 611-0011, Japan. Electronic address:
The development of a cytosolic delivery strategy for biopharmaceuticals is one of the central issues in drug development. Knowledge of the mechanisms underlying these processes may also pave the way for the discovery of novel delivery systems. L17E is a an attenuated cationic amphiphilic lytic (ACAL) peptide developed by our research group that shows promise for cytosolic antibody delivery.
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