量研学術機関リポジトリ「QST-Repository」は、国立研究開発法人 量子科学技術研究開発機構に所属する職員等が生み出した学術成果（学会誌発表論文、学会発表、研究開発報告書、特許等）を集積しインターネット上で広く公開するサービスです。 Welcome to QST-Repository where we accumulates and discloses the academic research results(Journal Publications, Conference presentation, Research and Development Report, Patent, etc.) of the members of National Institutes for Quantum Science and Technology.
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N-(5-Fluoro-2-phenoxyphenyl)-N-(2-[131I]iodo-5-methoxybenzyl)acetamide: a potent iodinated radioligand for peripheral benzodiazepine receptor in brain
利用統計を見る
The peripheral benzodiazepine receptor (PBR) density was increased in the injured brain and this increase has been used as an indicator of neuronal damage and several neurodenerative disorders such as Alzheimer's disease.We have previously developed two PET ligands [11C]DAA1106 and [18F]FEDAA1106 for PBR imaging in the human brain.Using DAA1106 as a lead compound, we designed two novel iodinated ligands: N-(5-fluoro-2-phenoxyphenyl)-N-(2-iodo-5-methoxybenzyl)acetamide (1) and N-(2,5-dimethoxybenzyl)-N-(5-iodo-2-phenoxyphenyl)acetamide (2).Here,we report the chemical synthesis and in vitro binding affinities of 1 and 2 to PBR, labeling of 1 and 2 using [131I]I, and distribution of [131I]1 and [131I]2 in the rat brain.
会議概要（会議名, 開催地, 会期, 主催者等）
EANM'06 Annual Congress of The European Association of Nuclear Medicine
N-(5-Fluoro-2-phenoxyphenyl)-N-(2-[131I]iodo-5-methoxybenzyl)acetamide: a potent iodinated radioligand for peripheral benzodiazepine receptor in brain
