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A method to predict the ratio of the tracer conversion rate to the tracer back-diffusion rate of an irreversible-type radiotracer in humans by preclinical evaluation
https://repo.qst.go.jp/records/46461
https://repo.qst.go.jp/records/4646188003123-a621-4206-b70a-4d0b36c1227f
Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2012-12-04 | |||||
タイトル | ||||||
タイトル | A method to predict the ratio of the tracer conversion rate to the tracer back-diffusion rate of an irreversible-type radiotracer in humans by preclinical evaluation | |||||
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 |
Ohya, Tomoyuki
× Ohya, Tomoyuki× Zhang, Ming-Rong× Fukumura, Toshimitsu× Fukushi, Kiyoshi× Kikuchi, Tatsuya× Irie, Toshiaki× 大矢 智幸× 張 明栄× 福村 利光× 福士 清× 菊池 達矢× 入江 俊章 |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Objective: The aim of this study was to develop a method to predict a tracer's alpha-value in the human brain on the basis of animal data. The alpha-value is the ratio of the conversion rate and the back-diffusion rate (k3/k2) and is one of the critical kinetic features of the detection sensitivity of target molecule activity, such as enzyme activity, in the measurement of PET and single-photon emission computed tomography using an irreversible-type radiotracer. Method: The alpha-value in the rat brain was estimated by a simultaneous assay of the tracer uptake and the target biochemical activity using N-[14C]-methylpiperidin-4-yl acetate ([14C]MP4A) and N-[14C]-methylpiperidin-4-yl propionate ([14C]MP4P) as test tracers, both of which are metabolic trapping tracers for measurement of brain acetylcholinesterase. The alpha-value in humans was then extrapolated from the alpha-value in rats by considering the differences between the species. The predicted human alpha-values were compared with those obtained from the kinetic analyses of human PET studies using [11C]MP4A and [11C]MP4P. Result: The alpha-values in the human brain cortex were predicted to be 0.51+/-0.1 for MP4A and 0.25+/-0.05 for MP4P. These results were close to values reported in other PET studies: 0.48+/-0.1 to 0.73+/-0.2 for MP4A and 0.15+/-0.04 to 0.18+/-0.04 for MP4P. Conclusion: The alpha-value predicted by this method would be used for practical selection or development of irreversible-type radiotracers for human use. |
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書誌情報 |
Nuclear Medicine Communications 巻 33, 号 10, p. 1019-1023, 発行日 2012-09 |
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ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0143-3636 | |||||
DOI | ||||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1097/mnm.0b013e328356fbc3 |