Nicotinic acetylcholine receptor subtype expression, function, and pharmacology: Therapeutic potential of α-conotoxins

Pharmacol Res. 2023 May:191:106747. doi: 10.1016/j.phrs.2023.106747. Epub 2023 Mar 30.

Abstract

The pentameric nicotinic acetylcholine receptors (nAChRs) are typically classed as muscle- or neuronal-type, however, the latter has also been reported in non-neuronal cells. Given their broad distribution, nAChRs mediate numerous physiological and pathological processes including synaptic transmission, presynaptic modulation of transmitter release, neuropathic pain, inflammation, and cancer. There are 17 different nAChR subunits and combinations of these subunits produce subtypes with diverse pharmacological properties. The expression and role of some nAChR subtypes have been extensively deciphered with the aid of knock-out models. Many nAChR subtypes expressed in heterologous systems are selectively targeted by the disulfide-rich α-conotoxins. α-Conotoxins are small peptides isolated from the venom of cone snails, and a number of them have potential pharmaceutical value.

Keywords: Cone snail; Nicotinic acetylcholine receptor; Peptide; α-conotoxin.

MeSH terms

  • Cell Membrane / metabolism
  • Conotoxins* / chemistry
  • Conotoxins* / metabolism
  • Conotoxins* / pharmacology
  • Neurons / metabolism
  • Nicotinic Antagonists / pharmacology
  • Nicotinic Antagonists / therapeutic use
  • Peptides / pharmacology
  • Receptors, Nicotinic* / metabolism

Substances

  • Conotoxins
  • Receptors, Nicotinic
  • Peptides
  • Nicotinic Antagonists