Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha6( *) subtype.
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ABSTRACT:
SUBMITTER: Breining SR
PROVIDER: S-EPMC6107347 | biostudies-literature | 2009 Aug
REPOSITORIES: biostudies-literature
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Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha6( *) subtype.
Breining Scott R SR Bencherif Merouane M Grady Sharon R SR Whiteaker Paul P Marks Michael J MJ Wageman Charles R CR Lester Henry A HA Yohannes Daniel D
Bioorganic & medicinal chemistry letters 20090527 15
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 alpha6 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 cess ...[more]
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