Author/Authors :
Daniele Simoni، نويسنده , , Marinella Roberti، نويسنده , , Riccardo Rondanin، نويسنده , , Riccardo Baruchello، نويسنده , , Marcello Rossi and Sabrina Selvi ، نويسنده , , Francesco Paolo Invidiata، نويسنده , , Stefania Merighi، نويسنده , , Katia Varani، نويسنده , , Stefania Gessi، نويسنده , , Pier Andrea Borea، نويسنده , , Silvia Marino، نويسنده , , Sabrina Cavallini، نويسنده , , Clementina Bianchi، نويسنده , , Anna Siniscalchi، نويسنده ,
Abstract :
6-Methoxylated and 8-oxygenated benztropines were prepared and evaluated for their DAT and SERT activity (binding and uptake inhibition). Methoxylation at the two-carbon bridge of benztropine produced a novel class of potent and selective DAT ligands. An interesting enantioselectivity was also observed for this new class of chiral benztropines. The inactivity of the 8-oxygenated analogues seems to point out that, unlike cocaine and its analogues, interactions of benztropine ligands with DAT may be strongly governed by the nitrogen atom.
