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We developed a new PET radioligand, (11)C-AC-N-benzyl-N-ethyl-2-(7-methyl-8-oxo-2-pheyl-7,8-dihydro-9H-purin-9-yl)acetamide ((11)C-AC-5216), that allows the imaging and quantification of PBRs in monkey and mouse brains. The aim of this study was to evaluate a quantification method of (11)C-AC-5216 binding in the human brain. METHODS: A 90-min dynamic PET scan was obtained for each of 12 healthy men after an intravenous injection of (11)C-AC-5216. Regions of interest were drawn on several brain regions. Binding potential, compared with nondisplaceable uptake (BPND), was calculated by a nonlinear least-squares fitting (NLS) method with the 2-tissue-compartment model, and total volume of distribution (VT) was estimated by NLS and graphical analysis methods. RESULTS: BPND was highest in the thalamus (4.6 +/- 1.0) and lowest in the striatum (3.5 +/- 0.7). VT obtained by NLS or graphical analysis showed regional distribution similar to BPND. However, there was no correlation between BPND and VT because of the interindividual variation of K1/k2. BPND obtained with data from a scan time of 60 min was in good agreement with that from a scan time of 90 min (r = 0.87). CONCLUSION: Regional distribution of (11)C-AC-5216 was in good agreement with previous PET studies of PBRs in the human brain. BPND is more appropriate for estimating (11)C-AC-5216 binding than is VT because of the interindividual variation of K1/k2. 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Quantitative Analysis of Peripheral Benzodiazepine Receptor in the Human Brain Using PET with 11C-AC-5216
https://repo.qst.go.jp/records/45711
https://repo.qst.go.jp/records/4571107f078b8-a66e-46d1-97dc-48315fa22798
Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2010-01-05 | |||||
タイトル | ||||||
タイトル | Quantitative Analysis of Peripheral Benzodiazepine Receptor in the Human Brain Using PET with 11C-AC-5216 | |||||
言語 | ||||||
言語 | eng | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
アクセス権 | ||||||
アクセス権 | metadata only access | |||||
アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
著者 |
Miyoshi, Michie
× Miyoshi, Michie× Ito, Hiroshi× Arakawa, Ryosuke× Takahashi, Hidehiko× Takano, Harumasa× Higuchi, Makoto× Okumura, Masaki× Otsuka, Tatsui× Kodaka, Fumitoshi× Sekine, Mizuho× Sasaki, Takeshi× Fujie, Saori× Seki, Chie× Maeda, Jun× Nakao, Ryuji× Zhang, Ming-Rong× Fukumura, Toshimitsu× Suhara, Tetsuya× et.al× 三好 美智恵× 伊藤 浩× 荒川 亮介× 高橋 英彦× 高野 晴成× 樋口 真人× 奥村 正紀× 大塚 達以× 小高 文聰× 関根 瑞保× 佐々木 健至× 藤江 沙織× 関 千江× 前田 純× 中尾 隆士× 張 明栄× 福村 利光× 須原 哲也 |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Peripheral benzodiazepine receptor (PBR) is upregulated in activated glial cells and is therefore a useful biomarker for inflammation in the brain and neurodegenerative disorders. We developed a new PET radioligand, (11)C-AC-N-benzyl-N-ethyl-2-(7-methyl-8-oxo-2-pheyl-7,8-dihydro-9H-purin-9-yl)acetamide ((11)C-AC-5216), that allows the imaging and quantification of PBRs in monkey and mouse brains. The aim of this study was to evaluate a quantification method of (11)C-AC-5216 binding in the human brain. METHODS: A 90-min dynamic PET scan was obtained for each of 12 healthy men after an intravenous injection of (11)C-AC-5216. Regions of interest were drawn on several brain regions. Binding potential, compared with nondisplaceable uptake (BPND), was calculated by a nonlinear least-squares fitting (NLS) method with the 2-tissue-compartment model, and total volume of distribution (VT) was estimated by NLS and graphical analysis methods. RESULTS: BPND was highest in the thalamus (4.6 +/- 1.0) and lowest in the striatum (3.5 +/- 0.7). VT obtained by NLS or graphical analysis showed regional distribution similar to BPND. However, there was no correlation between BPND and VT because of the interindividual variation of K1/k2. BPND obtained with data from a scan time of 60 min was in good agreement with that from a scan time of 90 min (r = 0.87). CONCLUSION: Regional distribution of (11)C-AC-5216 was in good agreement with previous PET studies of PBRs in the human brain. BPND is more appropriate for estimating (11)C-AC-5216 binding than is VT because of the interindividual variation of K1/k2. (11)C-AC-5216 is a promising PET ligand for quantifying PBR in the human brain. | |||||
書誌情報 |
Journal of Nuclear Medicine 巻 50, 号 7, p. 1095-1101, 発行日 2009-06 |
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ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0161-5505 | |||||
DOI | ||||||
識別子タイプ | DOI | |||||
関連識別子 | 10.2967/jnumed.109.062554 |