Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 15, Issue 12, Pages 2974-2979Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.04.036
Keywords
alpha 4 beta 2 nicotinic receptor; nAChR; partial agonist; smoking; cessation; alkaloid
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The preparation and biological activity of analogs of (-)-cytisine, an alpha 4 beta 2 nicotinic receptor partial agonist, are discussed. All-carbon-containing phenyl ring replacements of the pyridone ring system, generated via Heck cyclization protocols, exhibited weaker affinity and lower efficacy partial agonist profiles relative to (-)-cytisine. In vivo, selected compounds exhibit lower efficacy partial agonist profiles than that of (-)-cytisine. (c) 2005 Elsevier Ltd. All rights reserved.
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