Title : Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors - Wei_2004_Bioorg.Med.Chem.Lett_14_1855 |
Author(s) : Wei ZL , Xiao Y , Kellar KJ , Kozikowski AP |
Ref : Bioorganic & Medicinal Chemistry Lett , 14 :1855 , 2004 |
Abstract :
A series of bivalent ligands 6a-d of epibatidine were synthesized. All four ligands showed nanomolar binding affinities at six neuronal nicotinic acetylcholine receptor (nAChR) subtypes in competition binding assays. In contrast to epibatidine, these bivalent ligands are weak partial agonists at the alpha3beta4 nAChR as shown by functional assays. |
PubMedSearch : Wei_2004_Bioorg.Med.Chem.Lett_14_1855 |
PubMedID: 15050615 |
Wei ZL, Xiao Y, Kellar KJ, Kozikowski AP (2004)
Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors
Bioorganic & Medicinal Chemistry Lett
14 :1855
Wei ZL, Xiao Y, Kellar KJ, Kozikowski AP (2004)
Bioorganic & Medicinal Chemistry Lett
14 :1855