Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter

…, VA Parrino, TA Kopajtic, MJ Kuhar

文献索引：Houlihan, William J.; Boja, John W.; Parrino, Vincent A.; Kopajtic, Theresa A.; Kuhar, Michael J. Journal of Medicinal Chemistry, 1996 , vol. 39, # 25 p. 4935 - 4941

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被引用次数: 32

摘要

A series of halogenated (F, Cl, Br, I), pyrimido and diazepino homologs of mazindol were prepared and evaluated for their ability to displace [3H] WIN 35,428 binding and to inhibit uptake of [3H] dopamine (DA) in rat striatal tissue. All of the compounds except for the 2'- chloro (6) and 2'-bromo (16) analogs of mazindol displaced [3H] WIN 35,428 binding and inhibited [3H] DA uptake more effectively than (R)-cocaine. Structure-activity studies ...