Department of Molecular and Cell Biology, University of California, Berkeley, California 94720, USA.
ACS Chem Neurosci. 2011 Sep 21;2(9):536-43. doi: 10.1021/cn200037p. Epub 2011 Jun 9.
Photochromic channel blockers provide a conceptually simple and convenient way to modulate neuronal activity with light. We have recently described a family of azobenzenes that function as tonic blockers of K(v) channels but require UV-A light to unblock and need to be actively switched by toggling between two different wavelengths. We now introduce red-shifted compounds that fully operate in the visible region of the spectrum and quickly turn themselves off in the dark. Furthermore, we have developed a version that does not block effectively in the dark-adapted state, can be switched to a blocking state with blue light, and reverts to the inactive state automatically. Photochromic blockers of this type could be useful for the photopharmacological control of neuronal activity under mild conditions.
光致变色通道阻断剂为用光调节神经元活动提供了一种概念简单、方便的方法。我们最近描述了一类偶氮苯，它们作为 K(v) 通道的持续阻断剂起作用，但需要使用 UV-A 光来解除阻断，并需要通过在两个不同波长之间切换来主动切换。我们现在引入了完全在光谱可见光区域内工作的红移化合物，并在黑暗中迅速关闭。此外，我们开发了一种在暗适应状态下不能有效阻断的版本，可以用蓝光切换到阻断状态，并自动恢复到非活跃状态。这种类型的光致变色阻断剂可用于在温和条件下对神经元活动进行光药理控制。
