Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction

…, AC Mills, JA Holleman, SA Wolckenhauer…

Index: Carroll, F. Ivy; Blough, Bruce E.; Abraham, Philip; Mills, Andrew C.; Holleman, J. Ashley; Wolckenhauer, Scott A.; Decker, Ann M.; Landavazo, Antonio; McElroy, K. Timothy; Navarro, Hernan A.; Gatch, Michael B.; Forster, Michael J. Journal of Medicinal Chemistry, 2009 , vol. 52, # 21 p. 6768 - 6781

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Citation Number: 61

Abstract

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 [3H] dopamine ([3H] DA),[3H] serotonin ([3H] 5HT), and [3H] norepinephrine ([3H] NE) uptake inhibition studies, and by binding studies at the dopamine, serotonin, ...