Maziere B, Loc'h C, Stulzaft O, Hantraye P, Ottaviani M, Comar D, Maziere M
Eur J Pharmacol. 1986 Aug 15;127(3):239-47. doi: 10.1016/0014-2999(86)90370-5.
Bromolisuride, an ergoline derivative, was labeled with the positron emitter radionuclide, bromine 76. In vitro and in vivo binding and competition studies in rats demonstrated a high affinity (KD = 0.3 nM) and a high specificity of this new radioligand for D-2 dopamine receptors. PET kinetic studies in baboons showed an accumulation of [76Br]bromolisuride in the striatum which reached a maximum 30 min post-injection and which could be displaced by haloperidol. All these results indicated that this new ligand is certainly suitable for the non-invasive in vivo quantitative imaging of D-2 dopamine receptor sites in human brain.
溴麦角环肽，一种麦角灵衍生物，用正电子发射体放射性核素溴76进行标记。在大鼠身上进行的体外和体内结合及竞争研究表明，这种新的放射性配体对D-2多巴胺受体具有高亲和力（KD = 0.3 nM）和高特异性。在狒狒身上进行的PET动力学研究显示，[76Br]溴麦角环肽在纹状体中积聚，在注射后30分钟达到最大值，并且可被氟哌啶醇取代。所有这些结果表明，这种新的配体肯定适用于人脑D-2多巴胺受体位点的无创体内定量成像。
