Title of article
In pursuit of α4β2 nicotinic receptor partial agonists for smoking cessation: Carbon analogs of (−)-cytisine
Author/Authors
Jotham W. Coe، نويسنده , , Michael G. Vetelino، نويسنده , , Crystal G. Bashore، نويسنده , , Michael C. Wirtz، نويسنده , , Paige R. Brooks، نويسنده , , Eric P. Arnold، نويسنده , , Lorraine A. Lebel، نويسنده , , Carol B. Fox، نويسنده , , Steven B. Sands، نويسنده , , Thomas I. Davis، نويسنده , , David W. Schulz، نويسنده , , Hans Rollema، نويسنده , , F. David Tingley III، نويسنده , , Brian T. O’Neill، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
2974
To page
2979
Abstract
The preparation and biological activity of analogs of (−)-cytisine, an α4β2 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.
Keywords
?4?2 Nicotinic receptor , nAChR , Partial agonist , Alkaloid , smoking cessation
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795708
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