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Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the α6 subtype

Breining, Scott R. and Bencherif, Merouane and Grady, Sharon R. and Whiteaker, Paul and Marks, Michael J. and Wageman, Charles R. and Lester, Henry A. and Yohannes, Daniel (2009) Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the α6 subtype. Bioorganic and Medicinal Chemistry Letters, 19 (15). pp. 4359-4363. ISSN 0960-894X. PMCID PMC6107347. doi:10.1016/j.bmcl.2009.05.085.

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Direct comparison of pyridine versus pyrimidine substituents on a small but diverse set of ligands indicates that the pyrimidine substitution has the potential to enhance affinity and/or functional activity at α6 subunit-containing neuronal nicotinic receptors (NNRs) and decrease activation of ganglionic nicotinic receptors, depending on the scaffold. The ramifications of this structure–activity relationship are discussed in the context of the design of small molecules targeting smoking cessation.

Item Type:Article
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URLURL TypeDescription CentralArticle
Lester, Henry A.0000-0002-5470-5255
Additional Information:© 2009 Elsevier Ltd. Received 16 March 2009; revised 15 May 2009; accepted 20 May 2009. Available online 27 May 2009. This work was supported by NCDDG grant DA019375 from the National Institutes of Health to H.A.L., M.J.M. and M.B.
Funding AgencyGrant Number
Subject Keywords:Neuronal nicotinic receptor; NNR; Alpha 6; a3b4; SAR; Pyrimidine; Nicotinic acetylcholine receptor; Smoking cessation; Nicotine addiction; Dopamine release; Parkinson’s disease
Issue or Number:15
PubMed Central ID:PMC6107347
Record Number:CaltechAUTHORS:20090730-103918926
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Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:14738
Deposited By: Jason Perez
Deposited On:07 Aug 2009 18:35
Last Modified:08 Nov 2021 23:14

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