[EN] COMPOUNDS AS RADIOLIGANDS FOR THE DIAGNOSIS OF DISEASE<br/>[FR] COMPOSES UTILISES COMME LIGANDS RADIOACTIFS POUR DIAGNOSTIQUER UNE MALADIE
申请人:UPJOHN CO
公开号:WO2004052889A1
公开(公告)日:2004-06-24
Radiolabeled ligands useful as probes for determining the relative abundance, receptor occupancy, and/or function of nicotinic acetylcholine receptors. The compounds of Formula I as described herein are labeled with a radioactive isotopic moiety such as 11C, 18F, 76Br, 123I or 125I. Disorders are diagnosed by administering to a mammal a detectably labeled compound and detecting the binding of that compound to the nAChR. The compounds that have been administered are detected using methods including, but not limited to, position emission topography and single-photon to emission computed tomography. The present invention is useful in diagnosing a wide variety of diseases and disorders as discussed herein.
放射性标记的配体可用作探针,用于确定尼古丁乙酰胆碱受体的相对丰度、受体占有率和/或功能。本文描述的式I化合物标记有放射性同位素基团,如11C、18F、76Br、123I或125I。通过向哺乳动物注射可检测标记的化合物,并检测该化合物与nAChR的结合来诊断疾病。已经注射的化合物可使用包括但不限于正电子发射断层扫描和单光子发射计算机断层扫描在内的方法进行检测。本发明在诊断各种疾病和障碍方面具有实用性,如本文所述。