Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha6( *) subtype.

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 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 cessation.

SUBMITTER: Breining SR 

PROVIDER: S-EPMC6107347 | biostudies-literature | 2009 Aug

REPOSITORIES: biostudies-literature