Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai, 200237, China.
State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai, 200237, China.
Photochem Photobiol Sci. 2020 Jun;19(6):854-857. doi: 10.1039/d0pp00045k. Epub 2020 Oct 27.
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 (Periptaneta americana) DUM neurons. This light-responsive meta-diamide-based GABAR ligand allows for optical regulation of insecticidal activity and DUM neurons.
光药理学为配体活性和受体功能的时空控制提供了简便的解决方案。间二酰胺类杀虫剂作为一种拮抗剂作用于昆虫 GABA 受体 (GABARs)，导致神经元放电。我们在此通过将光致变色的偶氮苯与间二酰胺结合，提出了光致变色的 GABA 受体配体偶氮苯间二酰胺 (ABMDA)。ABMDA 表现出良好的互变异构效率和抗疲劳性。其中，ABMDA7 在紫外线照射前后对蚊子幼虫（白纹伊蚊）的杀虫活性差异为 1.5 倍。我们将这种光依赖性活性差异转化为美洲大蠊（Periptaneta americana）DUM 神经元膜电位的光学调制。这种对光响应的基于间二酰胺的 GABA 受体配体允许对杀虫活性和 DUM 神经元进行光学调节。
