Recent developments in neuronal nicotinic acetylcholine receptor antagonists

L. P. Dwoskin, R. Xu, J. T. Ayers, P. A. Crooks

Research output: Contribution to journalReview articlepeer-review

43 Scopus citations


Neuronal nicotinic acetylcholine receptors (nAChRs) belong to a superfamily of ligand-gated ion channel receptors and are distributed extensively throughout the central and peripheral nervous systems. The structural and functional diversity of these receptors has stimulated interest in the development of subtype-selective agonists, as a result of a greater understanding of the role of these receptors in neuropathology and disease, including Alzheimer's and Parkinson's disease, Tourette's syndrome, drug addiction and pain. Surprisingly, much less attention has been focused on the development of subtype-selective antagonists, which may also be useful as therapeutic agents. This article reviews the published patent literature on neuronal nicotinic receptor antagonists, with particular attention to receptor subtype selectivity of novel compounds that have been recently disclosed in the patent literature.

Original languageEnglish
Pages (from-to)1561-1581
Number of pages21
JournalExpert Opinion on Therapeutic Patents
Issue number10
StatePublished - 2000


  • Acetylcholine receptor
  • Alzheimer's disease
  • Anabaseine
  • Anabasine
  • Conotoxin
  • Dihydro-β-erythroidine
  • Drug abuse
  • GTS-21
  • Lobeline
  • Mecamylamine
  • NDNI
  • NONI
  • Neuronal nicotinic cholinergic channel blockers
  • Nicotine
  • Parkinson's disease

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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