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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

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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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