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J Med Chem. 2003 Jun 19;46(13):2716-30.

Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents.

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  • 1Department of Chemistry, University of Vermont, Burlington, Vermont 05405, USA.


Variation of the methoxycarbonyl and C-18 substituents of the antiaddictive compound 18-methoxycoronaridine, and contraction of its isoquinuclidine ring segment, provided 15 congeners for SAR evaluation at opioid and alpha3beta4 nicotinic acetylcholine receptors. The opioid activities were relatively low, and the alpha3beta4 nicotinic acetylcholine receptor activities were found to correlate with in vivo antiaddictive activities.

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