| Structure-Activity Studies of 7-Heteroaryl-3-azabicyclo[3.3.1]non-6-enes: A Novel Class of Highly Potent Nicotinic Receptor Ligands. | |
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MedLine Citation:
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PMID: 23025891 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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The potential for nicotinic ligands with affinity for the α4β2 or α7 subtypes to treat such diverse diseases as nicotine addiction, neuropathic pain, 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 analogs for activity at additional nicotinic subtypes. |
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Authors:
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Scott R Breining; Matthew S Melvin; Balwinder S Bhatti; Gary D Byrd; Melanie N Kiser; Christopher D Hepler; Dawn N Hooker; Jenny Zhang; Leslie A Reynolds; Lisa R Benson; Nikolai B Fedorov; Serguei S Sidach; J Pike Mitchener; Linda M Lucero; Ronald J Lukas; Paul Whiteaker; Daniel Yohannes |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-10-1 |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: - ISSN: 1520-4804 ISO Abbreviation: J. Med. Chem. Publication Date: 2012 Oct |
Date Detail:
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Created Date: 2012-10-2 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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