Synthesis of 18F labelled FK960, a candidate anti-dementia drug, and PET studies in conscious monkeys
✍ Scribed by Yoshihiro Murakami; Shintaro Nishimura; Akihiro Noda; Norihiro Harada; Hideo Tsukada
- Publisher
- John Wiley and Sons
- Year
- 2002
- Tongue
- French
- Weight
- 116 KB
- Volume
- 45
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.633
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✦ Synopsis
Abstract
The present study demonstrated the synthesis and in vivo study of ^18^F‐labeled N‐(4‐acetyl‐1‐piperazinyl)‐p‐fluorobenzamide (FK960) which is a novel anti‐dementia drug candidate. [^18^F]FK960 was prepared by a one‐pot, three reaction sequence, using nucleophilic fluorination, with an automated synthetic apparatus using either ethyl‐4‐trimethylammonium triflate (1a) or ethyl‐4‐nitrobenzoate (1b) as the precursor for labeling. Though 1a gave a higher yield, the specific activity was 50–100 fold higher with 1b. The radiochemical yield of [^18^F]FK960 was 7–15% (EOB) and the specific activity ranged from 2.0–60.2 GBq/μmol depending on the amount of F‐18 used. The synthesis time was 2.2–2.9 h. The obtained [^18^F]FK960 was injected into 3 conscious monkeys (100–120 MBq/kg body weight), and distribution images and pharmacokinetic data for [^18^F]FK960 showed similar uptake in different brain regions and 3‐fold higher levels of [^18^F]FK960 in blood relative to brain. Copyright © 2002 John Wiley & Sons, Ltd.