Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors

Zhi Liang Wei, Yingxian Xiao, Kenneth J. Kellar, Alan P. Kozikowski

Research output: Contribution to journalArticlepeer-review

Abstract

A series of bivalent ligands 6a-d of epibatidine were synthesized. All four ligands showed nanomolar binding affinities at six neuronal nicotinic acetylcholine receptor (nAChR) subtypes in competition binding assays. In contrast to epibatidine, these bivalent ligands are weak partial agonists at the α3β4 nAChR as shown by functional assays.

Original languageEnglish (US)
Pages (from-to)1855-1858
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number8
DOIs
StatePublished - Apr 19 2004

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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