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  • 02월 26일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제115회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Synthesis of deuterium substituted [18F]fluoromethyl-PBR28 and its preclinical comparison with [18F]fluoromethyl-PBR28

2015년 2월 12일 13시 29분 17초
MEDI.O-1 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
금 10시 : 00분
의약화학 - Oral Presentation for Young Medicinal Chemists
저자 및
문병석, 이병철*
분당서울대학교병원 핵의학과, Korea
N-(2-[18F]Fluoromethoxybenzyl)-N-(4-phenoxypyridin-3-yl)acetamide, ([18F]fluoromethyl-PBR28, [18F]1), sterically almost identical to [11C]PBR28 which was well known for TSPO specific radiotracer, was developed by our group for TSPO PET (positron emission tomography) imaging but [18F]1 had a little unstable in vivo due to probably defluorination. In this study, deuterium substituted [18F]fluoromethyl-PBR28-d2 ([18F]1-D) was synthesized to develop a PET radiotracer for enhanced in vivo stability and compared with [18F]1 in neuroinflammation rat models. [18F]1-D was synthesized by two-step reaction from CD2Br2, followed by the alkyation of desmethyl-PBR28. Comparison between [18F]1-D and [18F]1 was performed in in vitro and in vivo experiments. The radiochemical yield for [18F]1-D and [18F]1 were 12.4 and 35.8% with >185 GBq/umol of specific activity, respectively. In vitro binding affinity and log P showed similar values. In biodistribution, the uptakes of [18F]1-D and [18F]1 in femur had different pattern as time elapsed (2.1 vs 2.9 %ID/g at 5 min postinjection; 1.5 vs 4.1 %ID/g at 120 min postinjection, respectively), indicating that [18F]1-D was relatively stable in in vivo environment. In PET imaging studies, [18F]1-D was selectively accumulated in the ipsilateral striatum with high target-to-background ratio. BPND of [18F]1-D was about 1.4 times higher than that of [18F]1. The results presented here suggest that [18F]1-D hold promise as a neuroinflammation PET imaging agent in the field of brain disorders.