Optical Control of a Delayed Rectifier and a Two-Pore Potassium Channel with a Photoswitchable Bupivacaine

Philipp Leippe, Nils Winter, Martin Sumser, Dirk Trauner

Research output: Contribution to journalArticle

Abstract

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 feature 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.

Original languageEnglish (US)
JournalACS Chemical Neuroscience
DOIs
StateAccepted/In press - Jun 5 2018

Fingerprint

Potassium Channel Blockers
Potassium Channels
Bupivacaine
Local Anesthetics
Lighting
Action Potentials
Neurons
Light
Brain
Restoration
potassium channel protein TREK-1

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Cognitive Neuroscience
  • Cell Biology

Cite this

Optical Control of a Delayed Rectifier and a Two-Pore Potassium Channel with a Photoswitchable Bupivacaine. / Leippe, Philipp; Winter, Nils; Sumser, Martin; Trauner, Dirk.

In: ACS Chemical Neuroscience, 05.06.2018.

Research output: Contribution to journalArticle

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