CaltechAUTHORS
  A Caltech Library Service

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. https://resolver.caltech.edu/CaltechAUTHORS:20090730-103918926

[img] PDF - Accepted Version
See Usage Policy.

892Kb
[img] MS Word (Supplementary Data) - Supplemental Material
See Usage Policy.

36Kb

Use this Persistent URL to link to this item: https://resolver.caltech.edu/CaltechAUTHORS:20090730-103918926

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.


Item Type:Article
Related URLs:
URLURL TypeDescription
http://dx.doi.org/10.1016/j.bmcl.2009.05.085DOIArticle
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6107347PubMed CentralArticle
ORCID:
AuthorORCID
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.
Funders:
Funding AgencyGrant Number
NIHDA019375
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
Persistent URL:https://resolver.caltech.edu/CaltechAUTHORS:20090730-103918926
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:14738
Collection:CaltechAUTHORS
Deposited By: Jason Perez
Deposited On:07 Aug 2009 18:35
Last Modified:03 Oct 2019 00:52

Repository Staff Only: item control page