Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for α4β2nACh receptors
01 Pubblicazione su rivista
Deligia Francesco, Murineddu Gabriele, Gotti Cecilia, Ragusa Giulio, Fasoli Francesca, Sciaccaluga Miriam, Plutino Simona, Fucile Sergio, Loriga Giovanni, Asproni Battistina, Pinna Gerard A
ISSN: 0223-5234
The cholinergic pathways in the central nervous system (CNS) of animals and humans are important for cognitive and behavioural functions. Until a few years ago, it was thought that the key molecules transducing the cholinergic message were the metabotropic muscarinic receptors, but it is now known that ionotropic neuronal nicotinic receptors (nAChRs) are also involved. Based on recent studies, we prepared a small library of novel 3-substituted-3,6-diazabicyclo [3.1.1]heptanes, whose binding activity and functionality have been assayed. Among the synthesized compounds, the 3-(anilino)pyridine series resulted in the most interesting compounds with α4β2Kivalues ranging from 0.0225 nM (12g) to 2.06 nM (12o).