[EN] TRITIUM RADIOLABELING OF [3H]-1-CYCLOHEXYL-4-[3-(5-METHOXY-1,2, 3,4,-TETRAHYDRONAPHTHALEN-1-YL)-N-PROPYL]PIPERAZINE ([3H]-PB28), AS A POTENT SIGMA-2 RECEPTOR LIGAND<br/>[FR] RADIOMARQUAGE AU TRITIUM DE [3H]-1-CYCLOHEXYL-4-[3-(5- MÉTHOXY-1,2,3,4-TÉTRAHYDRONAPHTALÈN-1-YL)-N-PROPYL]PIPÉRAZINE ([3H]-PB28), EN TANT QUE LIGAND EFFICACE DES RÉCEPTEURS SIGMA-2
申请人:UNIV BARI
公开号:WO2009104058A1
公开(公告)日:2009-08-27
The invention relates to a novel process for the radiolabeling with [3H] of the l-cyclohexyl-4- [3- (5- methoxy-1, 2,3,4, -tetrahydronaphthalen-1-yl) -n- propyl]piperazine (PB28) ligand of formula 1 and enantiomeric forms thereof, specific for the sigma-2 receptors. The invention further relates to the same radiolabeled ligand and to its use as a highly selective analytical instrument in the evaluation of the expression levels of said receptors in tissues, as selection tool of novel specific ligands, and as diagnostic agent in diagnostic kits.
该发明涉及一种新型方法,用于对公式1中的l-环己基-4-[3-(5-甲氧基-1,2,3,4,-四氢萘基)-n-丙基]哌嗪(PB28)配体进行[3H]放射标记,以及其对映体形式,特异于sigma-2受体。该发明还涉及同一放射标记的配体及其用途,作为在组织中评估所述受体表达水平的高度选择性分析仪器,作为新型特异性配体的选择工具,并作为诊断试剂盒中的诊断试剂。