Neuronal Nicotinic Acetylcholine Receptor Structure and Function and Response to Nicotine

Int Rev Neurobiol. 2015;124:3-19. doi: 10.1016/bs.irn.2015.07.001. Epub 2015 Aug 21.


Nicotinic acetylcholine receptors (nAChRs) belong to the "Cys-loop" superfamily of ligand-gated ion channels that includes GABAA, glycine, and serotonin (5-HT3) receptors. There are 16 homologous mammalian nAChR subunits encoded by a multigene family. These subunits combine to form many different nAChR subtypes with various expression patterns, diverse functional properties, and differing pharmacological characteristics. Because cholinergic innervation is pervasive and nAChR expression is extremely broad, practically every area of the brain is impinged upon by nicotinic mechanisms. This review briefly examines the structural and functional properties of the receptor/channel complex itself. The review also summarizes activation and desensitization of nAChRs by the low nicotine concentrations obtained from tobacco. Knowledge of the three-dimensional structure and the structural characteristics of channel gating has reached an advanced stage. Likewise, the basic functional properties of the channel also are reasonably well understood. It is these receptor/channel properties that underlie the participation of nAChRs in nearly every anatomical region of the mammalian brain.

Keywords: Calcium permeability; Gating; Nicotine; Permeation; Presynaptic; Synaptic; nAChR.

Publication types

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

MeSH terms

  • Animals
  • Humans
  • Ion Channel Gating / drug effects
  • Ion Channel Gating / physiology*
  • Models, Molecular*
  • Nicotine / metabolism*
  • Nicotine / pharmacology
  • Protein Subunits / chemistry
  • Receptors, Nicotinic / chemistry*
  • Receptors, Nicotinic / metabolism*


  • Protein Subunits
  • Receptors, Nicotinic
  • Nicotine