Nicotinic acetylcholine receptors in neuropathic and inflammatory pain

FEBS Lett. 2018 Apr;592(7):1045-1062. doi: 10.1002/1873-3468.12884. Epub 2017 Oct 27.

Abstract

Nicotinic acetylcholine receptors (nAChRs) are actively being investigated as therapeutic targets for the treatment of pain and inflammation, but despite more than 30 years of research, there are currently no FDA-approved analgesics that are specific for these receptors. Much of the initial research effort focused on the α4β2 nAChR subtype, but more recently, additional subtypes have been identified as promising new leads and include α6β4, α7, and α9-containing nAChRs. This Review will focus on the distribution of these nAChRs in the cell types involved in neuropathic pain and inflammation and the activity of currently available nicotinic ligands.

Keywords: cancer pain; inflammatory pain; neuropathic pain; nicotinic acetylcholine receptors; α-conotoxin RgIA.

Publication types

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

MeSH terms

  • Analgesics / therapeutic use*
  • Animals
  • Humans
  • Inflammation / drug therapy
  • Inflammation / metabolism
  • Inflammation / pathology
  • Neuralgia* / drug therapy
  • Neuralgia* / metabolism
  • Neuralgia* / pathology
  • Receptors, Nicotinic / metabolism*

Substances

  • Analgesics
  • Receptors, Nicotinic