Department
neurobiology
Document Type
Article
Abstract
The potential for nicotinic ligands with affinity for the α4β2 or α7 subtypes to treat such diverse diseases as nicotine addiction, neuropathic pain, and neurodegenerative and cognitive disorders has been exhibited clinically for several compounds while preclinical activity in relevant in vivo models has been demonstrated for many more. For several therapeutic programs, we sought nicotinic ligands with various combinations of affinity and function across both subtypes, with an emphasis on dual α4β2-α7 ligands, to explore the possibility of synergistic effects. We report here the structure-activity relationships (SAR) for a novel series of 7-heteroaryl-3-azabicyclo[3.3.1]non-6-enes and characterize many of the analogues for activity at multiple nicotinic subtypes. © 2012 American Chemical Society.
Publication Date
11-26-2012
Publication Title
Journal of Medicinal Chemistry
ISSN
00222623
Volume
55
Issue
22
First Page
9929
Last Page
9945
Digital Object Identifier (DOI)
10.1021/jm3011299
Recommended Citation
Breining, Scott R.; Melvin, Matt; Bhatti, Balwinder S.; Byrd, Gary D.; Kiser, Melanie N.; Hepler, Christopher D.; Hooker, Dawn N.; Zhang, Jenny; Reynolds, Leslie A.; Benson, Lisa R.; Fedorov, Nikolai B.; Sidach, Serguei S.; Mitchener, J. Pike; Lucero, Linda M.; Lukas, Ronald J.; Whiteaker, Paul; and Yohannes, Daniel, "Structure-Activity Studies Of 7-Heteroaryl-3-Azabicyclo[3.3.1]Non-6-Enes: A Novel Class Of Highly Potent Nicotinic Receptor Ligands" (2012). Translational Neuroscience. 276.
https://scholar.barrowneuro.org/neurobiology/276