New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.
本文描述了结合到单胺转运体的新型替罗巴因类似物,特别是具有6-或7-取代基的8-氮杂、8-碳基和8-氧杂替罗巴因。本发明化合物可以是外消旋体,纯R-对映体或纯S-对映体。本发明的某些优选化合物具有对
DAT具有高选择性而不对
SERT具有选择性。还描述了制备药物治疗组合物,包括将化合物配制在药学可接受的载体中,以及通过将本发明的化合物与单胺转运体接触来抑制单胺转运体的5-羟
色胺重摄取的方法。本发明实践中的优选单胺转运体包括
多巴胺转运体、
血清素转运体和
去甲肾上腺素转运体。