Merging old and new perspectives on nicotinic acetylcholine receptors

Biochem Pharmacol. 2014 May 1;89(1):1-11. doi: 10.1016/j.bcp.2014.01.029. Epub 2014 Jan 31.


This review covers history underlying the discovery of the molecular mediators of nicotine's effects in the brain and the diversity of the nicotinic acetylcholine receptor (nAChR) subtypes. Models are presented for both their structure and their function as mediators of signal transduction, with special consideration of the differences between the two main subtypes: heteromeric receptors, which are specialized for rapid electrochemical signal transduction, and homomeric α7 receptors, which have come to be implicated in both ionotropic and metabotropic signaling. This review presents perspectives on the pharmacology and therapeutic targeting of nAChRs for the treatment of nicotine dependence or disease.

Keywords: Allosteric proteins; Electrophysiology; Molecular biology; Signal transduction; Synaptic function.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Models, Molecular
  • Protein Conformation
  • Receptors, Nicotinic / chemistry
  • Receptors, Nicotinic / drug effects*
  • Receptors, Nicotinic / metabolism
  • Signal Transduction


  • Receptors, Nicotinic