The specific aim of the project is to prepare a potent, selective inhibitor of the cocaine receptor at the dopamine transporter. This will be approached by structural modification of the clinically used Mazindol, a known inhibitor of the cocaine receptor. Inhibition of this receptor could result in a drug useful in blunting the craving for cocaine, a drug that has severe abuse problems in a wide spectrum of the United States population.
| Houlihan, William J; Ahmad, Umer F; Koletar, Judith et al. (2002) Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. J Med Chem 45:4110-8 |
| Barker, E L; Perlman, M A; Adkins, E M et al. (1998) High affinity recognition of serotonin transporter antagonists defined by species-scanning mutagenesis. An aromatic residue in transmembrane domain I dictates species-selective recognition of citalopram and mazindol. J Biol Chem 273:19459-68 |
| Houlihan, W J; Boja, J W; Parrino, V A et al. (1996) Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter. J Med Chem 39:4935-41 |
