| 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 |
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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 |
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