Adenosine A1 Receptor Mapping of the Human Brain by PET with 8-Dicyclopropylmethyl-1-11C-Methyl-3-Propylxanthine

Journal of Nuclear Medicine

Kenji Ishii¹  Yutaka Mori¹  Kiichi Ishiwata¹  Yuichi Kimura¹  Toru Sasaki¹  Keiichi Oda¹  Nobuyoshi Fukumitsu¹ 

关键词: 8-dicyclopropylmethyl-1-¹¹C-methyl-3-propylxanthine;    adenosine A₁ receptor;    brain;    PET;   

DOI  :  

学科分类：医学（综合）

来源: Society of Nuclear Medicine

【 摘 要 】

Adenosine is an endogenous modulator of synaptic functions in the central nervous system. To investigate the physiologic and pathologic roles of the adenosine receptors in the human brain, PET is a powerful in vivo technique. In this study, we quantitatively evaluated the distribution of a major subtype A1 adenosine receptor in the human brain by PET with a newly developed radioligand, 8-dicyclopropylmethyl-1-11C-methyl-3-propylxanthine (11C-MPDX). Methods: In 5 healthy volunteers, after PET measurement of the regional cerebral blood flow (rCBF) with 15O-H2O, a 60-min PET scan with 11C-MPDX was performed. The distribution volume (DV) of 11C-MPDX was quantitatively evaluated by Logan’s graphical analysis. Results: 11C-MPDX was taken up at a high level, reaching a peak at 2–2.5 min, followed by a rapid decrease. The unchanged form of 11C-MPDX in plasma was 75% at 60 min after injection. The DV of 11C-MPDX was large in the striatum and thalamus, moderate in the cerebral cortices and pons, and small in the cerebellum. The distribution pattern of 11C-MPDX in the brain was coincident with that of adenosine A1 receptors in vitro, reported previously, but discretely different from that of rCBF. Conclusion: 11C-MPDX PET has the potential for mapping adenosine A1 receptors in the human brain.

【 授权许可】

Unknown