Newman A H, Agoston G E
Psychobiology Section, National Institute on Drug Abuse - Intramural Research Program, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, Maryland 21224, USA.
Curr Med Chem. 1998 Aug;5(4):305-19.
The design, synthesis and pharmacological evaluation of novel dopamine transporter ligands, based on Benztropine [3a-(diphenylmethoxy) tropane], has been a focus of our research efforts toward the development of novel cocaine-abuse pharmacotherapeutics. Structure-activity relationships at the dopamine transporter, for this series of compounds, have been derived and compared to those of cocaine and GBR 12909. These studies suggest that structurally diverse dopamine uptake inhibitors may access different binding domains on the dopamine transporter. The distinctive behavioral profile displayed in this series of compounds, as compared to cocaine and other dopamine uptake inhibitors, is of particular interest and is proposed to be relevant to the pharmacodynamic and pharmacokinetic properties of this class of tropane-based molecules.
基于苯海索[3a-(二苯基甲氧基)托烷]的新型多巴胺转运体配体的设计、合成及药理评价，一直是我们开发新型可卡因滥用药物治疗方法研究工作的重点。已得出该系列化合物在多巴胺转运体上的构效关系，并与可卡因和GBR 12909的构效关系进行了比较。这些研究表明，结构多样的多巴胺摄取抑制剂可能作用于多巴胺转运体上不同的结合域。与可卡因和其他多巴胺摄取抑制剂相比，该系列化合物所表现出的独特行为特征尤为引人关注，并被认为与这类基于托烷的分子的药效学和药代动力学性质相关。
