IDENTIFICATION OF KAPPA-SELECTIVE ANALGESICS

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The National Institute on Drug Abuse has a continuing interest in supporting the development of a therapeutic compound for use in treating cocaine abuse. This project proposes to address the issue by the development of possible cocaine antagonists at the dopamine transporter site, which could potentially block the effects of cocaine. In Phase I, the contractor proposes to generate approximately 100-200 tropane derivatives as a "library" of novel compounds, using enzymatic-controlled processes, e.g., oxidation, reduction, hydrolysis, lactonization, epimerization, and acylation of the tropane ring system. The contractor will also perform in Phase I chemical structure characterization by mass spectrometry/gas chromatography, and, where indicated, stereochemical evaluation by nuclear magnetic resonance.