Addressing Motor Dysfunction by a Selective α6-Containing Nicotinic Receptor Antagonist

J Med Chem. 2023 Nov 9;66(21):14494-14496. doi: 10.1021/acs.jmedchem.3c01817. Epub 2023 Oct 18.

Abstract

In the striatum, presynaptic α6-containig nicotinic receptors are crucially involved in the modulation of dopamine release. CVN417, a novel selective antagonist at this receptor subtype, attenuates motor dysfunction in a Parkinson's disease-relevant animal model, suggesting, for this pathology, a therapeutic strategy that could greatly profit from the restricted localization of α6* nicotinic receptors in the brain.

MeSH terms

  • Animals
  • Brain / metabolism
  • Corpus Striatum
  • Dopamine / pharmacology
  • Nicotinic Antagonists / pharmacology
  • Nicotinic Antagonists / therapeutic use
  • Parkinson Disease* / drug therapy
  • Receptors, Nicotinic* / metabolism

Substances

  • Receptors, Nicotinic
  • Dopamine
  • Nicotinic Antagonists