SUMMARY Neuroreceptor imaging with radionuclide tracing in vivo has been greatly developed recently.Distribution,density,and activity of receptors in the brain can be visualized by the radioligands labeled for emission computed tomography(ECT),including PET(positron emission tomography)and SPECT(single photon emission computed tomography).The functional and quantitative imaging for several receptors,such as dopamine receptors,serotonin receptors,cholinergic receptors,benzodiazepine receptors,and opioid receptors,has clinical importance.The preparation of receptor imaging agents,foundation of the physio-mathematical model,and the development of nuclear medicine instruments are the main points.In the present review,we will concentrate on introducing the development of brain receptor imaging.
研制了一种适合单光子发射计算机断层(SPECT)显像用的阿片受体配基碘烷特培洛菲(7α O IA DPN),合成了阿片受体显像剂125I 7α O IA DPN,并检测了标记物的体外稳定性,进行了体内外结合实验研究。研制结果为:碘标记的7α O IA DPN放化纯度大于95%,标记率为81%～90%,比活度高达83.25PBq/mol,室温下放置24h,放化纯度仍大于90%。体外结合实验结果显示,其Kd=0.23nmol/L,Bmax为38pmol/g。研究结果表明,碘标记的7α O IA DPN有望成为SPECT的阿片受体显像剂。
