Chauveau Fabien, Boutin Hervé, Van Camp Nadja, Dollé Frédéric, Tavitian Bertrand
CEA, Institut d'Imagerie BioMédicale, Service Hospitalier Frédéric Joliot, Laboratoire d'Imagerie Moléculaire Expérimentale, Orsay, France.
Eur J Nucl Med Mol Imaging. 2008 Dec;35(12):2304-19. doi: 10.1007/s00259-008-0908-9. Epub 2008 Oct 1.
Neurodegenerative, inflammatory and neoplastic brain disorders involve neuroinflammatory reactions, and a biomarker of neuroinflammation would be useful for diagnostic, drug development and therapy control of these frequent diseases. In vivo imaging can document the expression of the peripheral benzodiazepine receptor (PBR)/translocator protein 18 kDa (TSPO) that is linked to microglial activation and considered a hallmark of neuroinflammation. The prototype positron emission tomography tracer for PBR, [(11)C]PK11195, has shown limitations that until now have slowed the clinical applications of PBR imaging. In recent years, dozens of new PET and SPECT radioligands for the PBR have been radiolabelled, and several have been evaluated in imaging protocols. Here we review the new PBR ligands proposed as challengers of [(11)C]PK11195, critically analyze preclinical imaging studies and discuss their potential as neuroinflammation imaging agents.
神经退行性、炎症性和肿瘤性脑疾病都涉及神经炎症反应，而神经炎症的生物标志物对于这些常见疾病的诊断、药物研发和治疗控制将是有用的。体内成像可以记录外周苯二氮䓬受体（PBR）/18 kDa转位蛋白（TSPO）的表达，该受体与小胶质细胞激活有关，并被认为是神经炎症的一个标志。用于PBR的正电子发射断层扫描示踪剂原型[(11)C]PK11195已显示出局限性，迄今为止，这些局限性减缓了PBR成像的临床应用。近年来，已有数十种用于PBR的新型正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）放射性配体被标记，并且有几种已在成像方案中进行了评估。在此，我们综述了被提议作为[(11)C]PK11195挑战者的新型PBR配体，批判性地分析临床前成像研究，并讨论它们作为神经炎症成像剂的潜力。
