Trifluoromethoxyl Substituted Phenylethylene Diamines as High Affinity s Receptor Ligands with Potent Anti-Cocaine Actions.

[摘要]：The phenylethylene diamines are a class of s receptor ligands with excellent selectivity over other biol. systems and with anti-cocaine actions that involve antagonism of s1 receptors. In order to increase the potency of the arom. methoxyl substituted analogs, trifluoromethoxyl groups were introduced to prevent metabolic demethylation. The para-substituted trifluoromethoxyl substituted analogs were shown to have increased s receptor affinity and represent the most potent anti-cocaine phenylethylene diamines yet described.

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