Photopharmacology offers facile solutions for spatiotemporal control over ligand activity and receptor function. The meta-diamide insecticide acts on insect GABA receptors (GABARs) as an antagonist that causes firing of a neuron. We present here photochromic GABAR ligands azobenzene-meta-diamides (ABMDAs) by incorporating photoswitchable azobenzene with meta-diamides. ABMDAs showed good isomerization efficiency and fatigue resistance. Among them, ABMDA7 shows a 1.5-fold insecticidal activity difference towards mosquito larvae (Aedes albopictus) before and after UV illumination. We translated this light-dependent activity difference to the optical modulation of the membrane potential of American cockroach (Periplaneta americana) DUM neurons. This light-responsive meta-diamide-based GABAR ligand allows for optical regulation of insecticidal activity and DUM neurons.

中文翻译：

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用于变体配体活性和神经元功能的光致变色间二酰胺。

光药理学为时空控制配体活性和受体功能提供了简便的解决方案。的间-二酰胺杀虫剂作用于昆虫GABA受体（GABARs）作为拮抗剂引起击发神经元。我们在这里介绍了光致变色GABAR配体偶氮苯-间二酰胺（ABMDAs），方法是将可光转换的偶氮苯与间-二酰胺结合在一起。ABMDAs表现出良好的异构化效率和抗疲劳性。其中，ABMDA7对蚊子幼虫（白纹伊蚊）的杀虫活性差异为1.5倍）在紫外线照射之前和之后。我们将这种依赖光的活性差异转化为美国蟑螂（Deri Neurota）DUM神经元膜电位的光学调节。这种基于光响应的基于间二酰胺的GABAR配体可对杀虫活性和DUM神经元进行光学调节。