Optical control of neuronal ion channels and receptors

Nat Rev Neurosci. 2019 Sep;20(9):514-532. doi: 10.1038/s41583-019-0197-2.


Light-controllable tools provide powerful means to manipulate and interrogate brain function with relatively low invasiveness and high spatiotemporal precision. Although optogenetic approaches permit neuronal excitation or inhibition at the network level, other technologies, such as optopharmacology (also known as photopharmacology) have emerged that provide molecular-level control by endowing light sensitivity to endogenous biomolecules. In this Review, we discuss the challenges and opportunities of photocontrolling native neuronal signalling pathways, focusing on ion channels and neurotransmitter receptors. We describe existing strategies for rendering receptors and channels light sensitive and provide an overview of the neuroscientific insights gained from such approaches. At the crossroads of chemistry, protein engineering and neuroscience, optopharmacology offers great potential for understanding the molecular basis of brain function and behaviour, with promises for future therapeutics.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Humans
  • Ion Channel Gating / drug effects
  • Ion Channel Gating / physiology
  • Ion Channels / antagonists & inhibitors
  • Ion Channels / chemistry
  • Ion Channels / metabolism*
  • Membrane Transport Modulators / pharmacology
  • Neurons / chemistry
  • Neurons / drug effects
  • Neurons / metabolism*
  • Optogenetics / methods
  • Optogenetics / trends*
  • Photochemical Processes* / drug effects
  • Receptors, G-Protein-Coupled / chemistry
  • Receptors, G-Protein-Coupled / metabolism*


  • Ion Channels
  • Membrane Transport Modulators
  • Receptors, G-Protein-Coupled