Published August 1, 2009
| Version Accepted Version + Supplemental Material
Journal Article
Open
Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the α6 subtype
Creators
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1.
Catalyst Biosciences (United States)
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2.
University of Colorado Boulder
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3.
California Institute of Technology
Abstract
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.
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.Attached Files
Accepted Version - nihms-128262.pdf
Supplemental Material - mmc1.doc
Files
nihms-128262.pdf
Additional details
Identifiers
- PMCID
- PMC6107347
- Eprint ID
- 14738
- Resolver ID
- CaltechAUTHORS:20090730-103918926
Funding
- NIH
- DA019375
Dates
- Created
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2009-08-07Created from EPrint's datestamp field
- Updated
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2021-11-08Created from EPrint's last_modified field