The challenges of modulating the 'rest and digest' system: acetylcholine receptors as drug targets

Drug Discov Today. 2017 Jan;22(1):97-104. doi: 10.1016/j.drudis.2016.09.011. Epub 2016 Sep 22.

Abstract

Acetylcholine, a major neurotransmitter of the parasympathetic and sympathetic nervous systems, was discovered in the early 1900s. Over the years, researchers have revealed much about its regulation, properties of its receptors and features of the downstream signaling that influence its terminal effects. The acetylcholine system, traditionally associated with neuromuscular communication, is now known to play a crucial part in modulation of the immune system and other 'rest and digest' effects. Recent research seeks to elucidate the system's role in brain functions including cognition, sleep, arousal, motivation, reward and pain. We highlight clinically approved and experimental drugs that modulate the acetylcholine receptors. The complexities in targeting the acetylcholine receptors are vast and finding future indications for drug development associated with specific acetylcholine receptors remains a challenge.

Publication types

  • Review

MeSH terms

  • Acetylcholine / genetics
  • Acetylcholine / metabolism*
  • Animals
  • Cholinergic Agonists / pharmacology*
  • Cholinergic Agonists / therapeutic use
  • Cholinergic Antagonists / pharmacology*
  • Cholinergic Antagonists / therapeutic use
  • Drug Discovery / methods*
  • Humans
  • Ligands
  • Molecular Targeted Therapy
  • Receptors, Cholinergic / genetics
  • Receptors, Cholinergic / metabolism*
  • Signal Transduction

Substances

  • Cholinergic Agonists
  • Cholinergic Antagonists
  • Ligands
  • Receptors, Cholinergic
  • Acetylcholine