Division of Radiological Sciences, Washington University School of Medicine, Mallinckrodt Institute of Radiology, Missouri 63110, USA.
Synapse. 2011 Aug;65(8):724-32. doi: 10.1002/syn.20891. Epub 2011 Mar 21.
A series of microPET imaging studies were conducted in anesthetized rhesus monkeys using the dopamine D₃-selective partial agonist, [¹⁸F]5. There was variable uptake in regions of brain known to express a high density of D₃ receptors under baseline conditions. Pretreatment with lorazepam (1 mg/kg, i.v. 30 min) to reduce endogenous dopamine activity before tracer injection resulted in a dramatic increase in uptake in the caudate, putamen, and thalamus, and an increase in the binding potential (BP) values, a measure of D₃ receptor binding in vivo. These data indicate that there is a high level of competition between [¹⁸F]5 and endogenous dopamine for D₃ receptors in vivo.
进行了一系列使用多巴胺 D₃ 选择性部分激动剂 [¹⁸F]5 的麻醉恒河猴 microPET 成像研究。在基线条件下，在已知表达高密度 D₃ 受体的脑区有可变的摄取。在示踪剂注射前用劳拉西泮（1 mg/kg，静脉注射 30 分钟）预处理以减少内源性多巴胺活性，导致尾状核、壳核和丘脑的摄取显著增加，并增加结合潜力（BP）值，这是体内 D₃ 受体结合的度量。这些数据表明，[¹⁸F]5 和内源性多巴胺之间存在高水平的竞争，用于体内的 D₃ 受体。
