Optical Control of a Delayed Rectifier and a Two-Pore Potassium Channel with a Photoswitchable Bupivacaine.,ACS Chemical Neuroscience

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Optical Control of a Delayed Rectifier and a Two-Pore Potassium Channel with a Photoswitchable Bupivacaine.
ACS Chemical Neuroscience ( IF 4.1 ) Pub Date : 2018-08-14 , DOI: 10.1021/acschemneuro.8b00279
Philipp Leippe ₁ , Nils Winter ₁ , Martin P Sumser ₁ , Dirk Trauner _{1,

2}

Affiliation

Photoswitchable blockers of potassium channels can be used to optically control neuronal excitability and hold great promise for vision restoration. Here, we report a series of improved photoswitchable blockers that are furnished with a new pharmacophore based on the local anesthetic bupivacaine. These azobupivacaines (ABs) enable optical control over the delayed rectifier channel Kv2.1. and target the two-pore domain potassium channel TREK-1. For the first time, we have identified a compound that blocks conductance in the dark and potentiates it upon illumination. Using light as a trigger, ABs efficiently and reversibly silence action potential firing of hippocampal neurons in acute mouse brain slices.

中文翻译：

具有光开关布比卡因的延迟整流器和两孔钾通道的光学控制。

钾离子通道的光开关阻滞剂可用于光学控制神经元兴奋性，并有望恢复视力。在这里，我们报告了一系列改进的可光转换阻滞剂，这些阻滞剂配备了基于局部麻醉的布比卡因的新药效基团。这些偶氮布比卡因（AB）可以对延迟的整流器通道Kv2.1进行光学控制。并靶向两孔结构域钾通道TREK-1。我们首次确定了一种化合物，该化合物可在黑暗中阻断电导，并在光照时增强电导。利用光作为触发因素，AB可有效且可逆地使急性小鼠脑切片中海马神经元的动作电位放电沉默。

更新日期：2018-07-12

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