In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine

In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine

The preparation and biological activity of analogs of (-)-cytisine, an alpha4beta2 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 par...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2005-06, Vol.15 (12), p.2974-2979
Hauptverfasser: Coe, Jotham W, Vetelino, Michael G, Bashore, Crystal G, Wirtz, Michael C, Brooks, Paige R, Arnold, Eric P, Lebel, Lorraine A, Fox, Carol B, Sands, Steven B, Davis, Thomas I, Schulz, David W, Rollema, Hans, Tingley, 3rd, F David, O'Neill, Brian T
Format: Artikel
Sprache:eng
Schlagworte:
Alkaloids - chemistry
Alkaloids - pharmacology
Animals
Azocines - chemistry
Azocines - pharmacology
Carbon - chemistry
Dopamine - metabolism
Nicotinic Agonists - chemistry
Nicotinic Agonists - pharmacology
Nucleus Accumbens - drug effects
Quinolizines - chemistry
Quinolizines - pharmacology
Rats
Receptors, Nicotinic - chemistry
Receptors, Nicotinic - metabolism
Smoking Cessation
Structure-Activity Relationship
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Zusammenfassung:The preparation and biological activity of analogs of (-)-cytisine, an alpha4beta2 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.
ISSN:0960-894X