MEDICINAL CHEMISTRY SYNTHESIS OF POTENTIAL TREATMENT

本合同的目的是设计和合成以下化合物 主要影响多巴胺能系统，并替代可卡因或 分析它的影响。该项目应包括以下任何一项的合成 以下：多巴胺摄取抑制剂的起效速度比 可卡因；通过抑制作用影响多巴胺能系统的化合物 多巴胺或5-羟色胺转运体 转运体选择性可卡因类似物；多巴胺部分激动剂；以及 抗激动剂；以及多巴胺节约型可卡因拮抗剂(化合物 与多巴胺转运体结合而不抑制摄取)；以及化合物 对D_1和D_3受体有选择性。该项目还应提供 有希望的化合物的放大生产和模拟合成。这个 该项目的主要目标是为NIDA提供一种新颖的资源 有可能用于治疗可卡因滥用的化合物。

The purpose of this contract is to design and synthesize compounds which affect primarily dopaminergic systems and either substitute for cocaine or anatagoize its effects. The project shall involve the synthesis of any of the following: dopamine uptake inhibitors with a slower rate of onset than cocaine; compound which affect dopaminergic systems through the inhibition of dopamine or serotonin transporters; serotonin transporters; serotonin transporter selective cocaine analogs; dopamine partial agonists, and anatagonists; and dopamine sparing cocaine antagoists (Compounds that bind to the dopamine transporter without inhibiting uptake); and compound selective for D1 and D3 receptors. The project shall also provide for the scale-up production, and analog synthesis, of promissing compounds. The major goal of this project is to provide NIDA with a resource of novel compounds with potential use in the treatment of cocaine abuse.