Wei_2005_J.Med.Chem_48_1721

Reference

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 - Wei_2005_J.Med.Chem_48_1721
Author(s) : Wei ZL , Xiao Y , Yuan H , Baydyuk M , Petukhov PA , Musachio JL , Kellar KJ , Kozikowski AP
Ref : Journal of Medicinal Chemistry , 48 :1721 , 2005
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.

PubMedSearch : Wei_2005_J.Med.Chem_48_1721
PubMedID: 15771418

Related information

Citations formats

Wei ZL, Xiao Y, Yuan H, Baydyuk M, Petukhov PA, Musachio JL, Kellar KJ, Kozikowski AP (2005)
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
Journal of Medicinal Chemistry 48 :1721

Wei ZL, Xiao Y, Yuan H, Baydyuk M, Petukhov PA, Musachio JL, Kellar KJ, Kozikowski AP (2005)
Journal of Medicinal Chemistry 48 :1721