Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity

Sheela K. Chellappan, Yingxian Xiao, Werner Tueckmantel, Kenneth J. Kellar, Alan P. Kozikowski

Research output: Contribution to journalArticlepeer-review

Abstract

We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the α4β2 nAChR subtype in binding assays than cytisine. The 9-vinyl derivative was found to have a very similar agonist activity profile to that of cytisine.

Original languageEnglish (US)
Pages (from-to)2673-2676
Number of pages4
JournalJournal of medicinal chemistry
Volume49
Issue number9
DOIs
StatePublished - May 4 2006

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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