Quantitative Analyses of 18F-FEDAA1106 Binding to Peripheral Benzodiazepine Receptors in Living Human Brain

Journal of Nuclear Medicine

Fumihiko Yasuno¹  Ryohei Matsumoto¹  Yoko Ikoma¹  Shoko Nozaki¹  Tetsuya Suhara¹  Nobumasa Kato¹  Kazutoshi Suzuki¹  Ryuji Nakao¹  Jun Kosaka¹  Hiroshi Ito¹  Miho Ota¹  Akihiro Takano¹  Yota Fujimura¹  Ming-Rong Zhang¹ 

关键词: ¹⁸F-FEDAA1106;    microglia;    peripheral benzodiazepine receptor;    binding potential;    PET;   

DOI  :  

学科分类：医学（综合）

来源: Society of Nuclear Medicine

【 摘 要 】

N-(5-Fluoro-2-phenoxyphenyl)-N-(2-18F-fluoroethyl-5-methoxybenzyl)acetamide (18F-FEDAA1106) is a potential PET ligand with highly selective and specific binding to peripheral benzodiazepine receptor (PBR). It has been reported that the regional density of PBR in the brain is increased in several neurodegenerative and psychiatric disorders. Thus, a reliable tracer method for evaluating PBR would be of use clinically and for research. To our knowledge, this is the first study to investigate the 18F-FEDAA1106 binding to PBR in living human brain by PET. We also aimed to evaluate various analytic methods to quantify the density of PBR. Methods: PET studies with 18F-FEDAA1106 were performed on 7 healthy men. Volumes of interest (VOIs) were drawn on PET images. In each VOI, binding potential (BP) was calculated by nonlinear least-squares (NLS) fitting based on the 2-tissue compartment model, and the distribution volume (DV) was also estimated by NLS, Logan plot, and multilinear analysis (MA) methods. To estimate errors in calculation of BP and DV, simulation studies were also performed. Results: The DVs estimated with each of the methods were significantly correlated. There was also significant correlation between BP with NLS and DV with NLS, Logan plot, or MA. But the interindividual differences in the distribution volume of the free and nonspecific binding compartment (K1/k2) were relatively large. In a simulation study, variation of the DV estimated by Logan plot was relatively small, but it was underestimated as the noise increased. By MA, the bias of DV was smaller, but the variation of DV was larger than by Logan plot. Within a 3% noise level, there was almost no difference between Logan plot and MA in both bias and variation. DVs estimated by both Logan plot and MA were underestimated by 10%–20%. Although the variation of DV was larger by NLS than by Logan plot, it was small enough in the noise level of VOI analysis, and the bias of DV was 0%–2%. Conclusion: The simulation studies indicated that NLS is a suitable method for the estimation of 18F-FEDAA1106 binding to PBRs.

【 授权许可】

Unknown