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A novel series of [3.2.1] azabicyclic biaryl ethers as α3β4 and α6/4β4 nicotinic receptor agonists

✍ Scribed by John A. Lowe III; Shari L. DeNinno; Jotham W. Coe; Lei Zhang; Scot Mente; Raymond S. Hurst; Robert J. Mather; Karen M. Ward; Alka Shrikhande; Hans Rollema; David E. Johnson; Weldon Horner; Roxanne Gorczyca; F. David Tingley III; Rouba Kozak; Mark J. Majchrzak; Theresa Tritto; Jen Sadlier; Chris L. Shaffer; Brenda Ellerbrock; Sarah M. Osgood; Mary C. MacDougall; Laura L. McDowell

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 243 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.06.142

No coin nor oath required. For personal study only.

✦ Synopsis

We report the synthesis of a series of [3.2.1]azabicyclic biaryl ethers as selective agonists of a3and a6-containing nicotinic receptors. In particular, compound 17a from this series is a potent a3b4 and a6/4b4 receptor agonist in terms of both binding and functional activity. Compound 17a also shows potent in vivo activity in CNS-mediated animal models that are sensitive to antipsychotic drugs.

Compound 17a may thus be a useful tool for studying the role of a3b4 and a6/4b4 nicotinic receptors in CNS pharmacology.

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