Synthesis and preliminary evaluation of [11C]KF17837, a selective adenosine A2A antagonist

✍ Scribed by Kiichi Ishiwata; Junko Noguchi; Hinako Toyama; Yojiro Sakiyama; Nobuaki Koike; Shin-Ichi Ishii; Keiichi Oda; Kazutoyo Endo; Fumio Suzuki; Michio Senda

• Publisher: Elsevier Science
• Year: 1996
• Tongue: English
• Weight: 371 KB
• Volume: 47
• Category: Article
• ISSN: 0969-8043
• DOI: 10.1016/0969-8043(95)00295-2

✦ Synopsis

An 11C-labeled selective adenosine A2A antagonist, (E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-[11C]-methylxanthine ([11C]KF17837), was prepared by reaction of (E)-8-(3,4-dimethoxystyryl)-1,3-dipropylxanthine and [11C]methyl iodide with decay-corrected radiochemical yield of 19-50%, radiochemical purity of > 99%, sp. act. of 17-100 GBq/mumol and preparation time of 20-25 min. In mice, the myocardium showed the highest (13.4% ID/g) at 5 min after i.v. injection, which decreased gradually with time. The specific myocardial uptake was visualized by gamma-camera. In the brain region the radioactivity level was higher in the A2A receptors-rich striatum than in the cortex and cerebellum. The specific striatal uptake in rats was clearly demonstrated by PET. These results have shown that [11C]KF17837 is a potential PET radioligand for mapping the adenosine A2A receptors in the heart and brain.