Journal of medicinal chemistry

Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo [3.2. 1] octane) dopamine uptake inhibitors

DI Kim, MM Schweri, HM Deutsch

Index: Kim, Deog-Il; Schweri, Margaret M.; Deutsch, Howard M. Journal of Medicinal Chemistry, 2003 , vol. 46, # 8 p. 1456 - 1464

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Citation Number: 20

Abstract

A series of 8-substituted-3-azabicyclo [3.2. 1] octanes (isotropanes) were synthesized and tested for inhibitor potency using [3H] WIN 35,428 binding at the dopamine (DA) transporter,[3H] citalopram binding at the serotonin (5-HT) transporter, and [3H] DA uptake assays. The synthesis started with a Mannich condensation of cyclopentanone, benzylamine, and fomaldehyde to afford N-benzyl-3-azabicyclo [3.2. 1] octan-8-one (6). ...