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).

Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for α4β2nACh receptors / Deligia, Francesco; Murineddu, Gabriele; Gotti, Cecilia; Ragusa, Giulio; Fasoli, Francesca; Sciaccaluga, Miriam; Plutino, Simona; Fucile, Sergio; Loriga, Giovanni; Asproni, Battistina; Pinna, Gerard A. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 152:(2018), pp. 401-416. [10.1016/j.ejmech.2018.04.026]

Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for α4β2nACh receptors

Sciaccaluga, Miriam;Plutino, Simona;Fucile, Sergio;
2018

Abstract

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).
2018
3,6-diazabicyclo[3.1.1] heptanes; Synthesis; Neuronal nicotinic acetylcholine receptors; α4β2selectivity; Agonism
01 Pubblicazione su rivista::01a Articolo in rivista
Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for α4β2nACh receptors / Deligia, Francesco; Murineddu, Gabriele; Gotti, Cecilia; Ragusa, Giulio; Fasoli, Francesca; Sciaccaluga, Miriam; Plutino, Simona; Fucile, Sergio; Loriga, Giovanni; Asproni, Battistina; Pinna, Gerard A. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 152:(2018), pp. 401-416. [10.1016/j.ejmech.2018.04.026]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/1112795
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