A graphical method to compare the in vivo binding potential of PET radioligands in the absence of a reference region: application to [C-11]PBR28 and [F-18]PBR111 for TSPO imaging

作者：Guo Qi^*; Owen David R; Rabiner Eugenii A; Turkheimer Federico E; Gunn Roger N

来源：Journal of Cerebral Blood Flow and Metabolism, 2014, 34(7): 1162-1168.

DOI：10.1038/jcbfm.2014.65

• graphical analysis
• PET
• radioligand comparison
• specific binding
• TSPO

Positron emission tomography (PET) radioligands for a reversible central nervous system (CNS) demand a high specific to nonspecific signal characterized by the binding potential (BPND). The quantification of BPND requires the determination of the nondisplaceable binding usually derived from a reference region devoid of the target of interest. However, for many CNS targets, there is no valid reference region available. In such cases, the total volume of distribution (V-T) is often used as the outcome measure, which includes both the specific and nonspecific binding signals. Here we present a graphical method that allows for direct comparison of the binding potential of ligands using the regional V-T data alone via linear regression. The method was first validated using literature data for five serotonin transporter ligands, for which a reference region exists, and then applied to two second generation 18 kDa translocator protein radioligands, namely [C-11]PBR28 and [F-18]PBR111. The analysis determined that [C-11]PBR28, had a higher BPND than [F-18]PBR111.

• 出版日期2014-7