Sadzot B, Frost J J
Johns Hopkins Medical Institutions, Baltimore, Maryland.
Anesth Prog. 1990 Mar-Jun;37(2-3):113-20.
Opiate receptors in the brain are the target of endogenous opioids and of exogenous synthetic opiates. These receptors play a major role in the modulation of pain perception. Using the appropriate ligands, positron emission tomography now allows investigators to monitor neuroreceptors in vivo. We have used (11)C-diprenorphine and the extremely potent mu opiate receptor agonist, (11)C-carfentanil, to image the distribution of opiate receptors in the brain and to quantify their density, their affinity, and their occupancy. Several important aspects of the in vivo opiate receptor labeling with positron emission tomography in relation to the study of pain are considered in this paper. Monitoring receptor occupancy by opiate drugs as a function of pain relief has the potential to reveal better ways to treat pain.
大脑中的阿片受体是内源性阿片类物质和外源性合成阿片的作用靶点。这些受体在疼痛感知的调节中起主要作用。利用合适的配体，正电子发射断层扫描现在使研究人员能够在体内监测神经受体。我们使用了（11）C-二丙诺啡和极强效的μ阿片受体激动剂（11）C-卡芬太尼，来成像大脑中阿片受体的分布，并量化其密度、亲和力和占有率。本文考虑了正电子发射断层扫描在体内标记阿片受体与疼痛研究相关的几个重要方面。监测阿片类药物对受体的占有率与疼痛缓解的关系，有可能揭示更好的疼痛治疗方法。
