公开(公告)号：US06180083B2

公开(公告)日：2001-01-30

申请号：US09180281

申请日：1998-11-10

申请人： Laurent Mauclaire ,  Patrick Emond ,  Denis Guilloteau ,  Jean-Claude Besnard ,  Yves Frangin

发明人： Laurent Mauclaire ,  Patrick Emond ,  Denis Guilloteau ,  Jean-Claude Besnard ,  Yves Frangin

IPC分类号： A61K5100

CPC分类号： C07D451/02 ,  A61K51/0448 ,  A61K2123/00

摘要： The present invention relates to tropane derivatives having particular use for the in vivo detection of dopamine transporters. These derivatives meet the formula in which R1 is I or Sn (R3)3, R2 is for example the methyl group, and X and Y are various substituents. The derivatives with X═CH3 and Y═H show strong specificity for the dopamine transporter compared with the serotonin transporter (74% inhibition when the transporter is previously saturated with GBR 12909).

摘要翻译： 本发明涉及特异性用于体内检测多巴胺转运蛋白的托烷衍生物。这些衍生物涉及R1为I或Sn（R3）3，R2为例如甲基的化合物，X和Y为各种取代基 具有X = CH 3和Y = H的衍生物与血清素转运蛋白相比显示出对多巴胺转运蛋白的强特异性（当转运蛋白先前用GBR12909饱和时，其抑制为74％）。