申请人:The Regents, University of California
公开号:US05372813A1
公开(公告)日:1994-12-13
Disclosed is a substituted 6-nitroquipazine of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each selected from the group consisting of H, Fl, CL, Br, I, CF.sub.3, CH.sub.2 CH.sub.2 F, CH.sub.3, CH.sub.2 CH.sub.3, and --CH(CH.sub.3).sub.2, and wherein one of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 is other than H. Also disclosed is a method for measurement of serotonin uptake sites in a sample, in which a radioligand is incubated with a sample and then the radioactivity of the radioligand bound to the sample is determined, utilizing a radio labeled substituted 6-nitroquipazine as the radioligand. Also disclosed is a method of manufacture and method of use.
本发明涉及一种化合物,即式子##STR1##的取代6-硝基奎佩嗪,其中R.sub.1、R.sub.2、R.sub.3和R.sub.4分别选自H、Fl、Cl、Br、I、CF.sub.3、CH.sub.2 CH.sub.2 F、CH.sub.3、CH.sub.2 CH.sub.3和--CH(CH.sub.3).sub.2的群体,其中R.sub.1、R.sub.2、R.sub.3和R.sub.4中的一个不是H。本发明还公开了一种用放射性标记的取代6-硝基奎佩嗪作为放射性配体,将放射性标记的配体与样品一起孵育,然后测定结合到样品中的放射性标记的配体的放射性,以测量样品中的5-羟色胺摄取位点的方法。本发明还公开了一种制造方法和使用方法。