Acid-sensing ion channels as potential therapeutic targets

Trends Pharmacol Sci. 2021 Dec;42(12):1035-1050. doi: 10.1016/ Epub 2021 Oct 18.


Tissue acidification is associated with a variety of disease states, and acid-sensing ion channels (ASICs) that can sense changes in pH have gained traction as possible pharmaceutical targets. An array of modulators, ranging from small molecules to large biopharmaceuticals, are known to inhibit ASICs. Here, we summarize recent insights from animal studies to assess the therapeutic potential of ASICs in disorders such as ischemic stroke, various pain-related processes, anxiety, and cardiac pathologies. We also review the factors that present a challenge in the pharmacological targeting of ASICs, and which need to be taken into careful consideration when developing potent and selective modulators in the future.

Keywords: animal models; ischemia; ligand-gated ion channel; pain; pharmacological targeting; stroke.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Acid Sensing Ion Channels* / chemistry
  • Animals
  • Humans


  • Acid Sensing Ion Channels