Pyridine alkylsulfone derivatives typified by oxazosulfyl (Sumitomo Chemical Company Ltd.) and compound (Syngenta) represent a new class of insecticides, with potent activity against several insect orders. Whilst the MOA of this class has been attributed to interaction with the voltage-gated sodium channel (VGSC), here we present strong evidence that their toxicity to insects is mediated primarily through inhibition of the vesicular acetylcholine transporter (VAChT). Alkylsulfone intoxication in insects is characterised by (i) a reduction in cholinergic synaptic transmission efficiency demonstrated by a depression of cercal afferent activity in giant-interneurone preparations of American cockroach (), (ii) selective block of cholinergic-transmission dependent post-synaptic potentials in the giant-fibre pathway and (iii) abolition of miniature excitatory post-synaptic currents (mEPSCs) in an identified synapse in larvae.

中文翻译：

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一类新型杀虫烷基砜是囊泡乙酰胆碱转运的有效抑制剂

以恶唑磺酰（住友化学有限公司）和化合物（先正达）为代表的吡啶烷基砜衍生物代表了一类新的杀虫剂，对多种昆虫具有有效的活性。虽然此类 MOA 归因于与电压门控钠通道 (VGSC) 的相互作用，但在这里我们提出强有力的证据，表明它们对昆虫的毒性主要是通过抑制囊泡乙酰胆碱转运蛋白 (VAChT) 介导的。昆虫中的烷基砜中毒的特征是（i）胆碱能突触传递效率降低，这通过美洲大蠊的巨型中间神经元制剂中尾部传入活性的抑制来证明（），（ii）选择性阻断胆碱能传递依赖的突触后电位（iii）在幼虫中已确定的突触中消除微型兴奋性突触后电流（mEPSC）。