F Ivy Carroll, Bruce E Blough, Philip Abraham, Andrew C Mills, J Ashley Holleman, Scott A Wolckenhauer, Ann M Decker, Antonio Landavazo, K Timothy McElroy, Hernán A Navarro, Michael B Gatch, Michael J Forster
A series of bupropion (1a) analogues (1b-1ff) were synthesized, and their in vitro and in vivo pharmacological properties evaluated with the goal of developing a 1a analogue that had better properties for treating addictions. Their in vitro pharmacological properties were examined by [(3)H]dopamine ([(3)H]DA), [(3)H]serotonin ([(3)H]5HT), and [(3)H]norepinephrine ([(3)H]NE) uptake inhibition studies, and by binding studies at the dopamine, serotonin, and norepinephrine transporters using [(125)I]RTI-55 in cloned transporters...
November 12, 2009: Journal of Medicinal Chemistry