Document Report Card

ID: ALA1142717

Journal: J Med Chem

Title: Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.

Authors: Wei ZL, Xiao Y, Yuan H, Baydyuk M, Petukhov PA, Musachio JL, Kellar KJ, Kozikowski AP.

Abstract: Introduction of a hydrophobic or hydrogen-bonding alkynyl group into the C5 position of the pyridyl ring of epibatidine and A-84543 significantly increased the selectivity for neuronal nicotinic acetylcholine receptors (nAChRs) containing beta2 subunits over nAChRs containing beta4 subunits (K(i) ratio up to 92000-fold). Our data indicate that the extracellular domains of the nAChRs are sufficiently different to allow for the design of novel ligands with high affinity and selectivity for the nAChR subtypes.

CiteXplore: 15771418

DOI: 10.1021/jm0492406