Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the α6∗ subtype

…, M Bencherif, SR Grady, P Whiteaker, MJ Marks…

Index: Breining, Scott R.; Bencherif, Merouane; Grady, Sharon R.; Whiteaker, Paul; Marks, Michael J.; Wageman, Charles R.; Lester, Henry A.; Yohannes, Daniel Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 15 p. 4359 - 4363

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Citation Number: 14

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 ...