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A First-in-human Study of 11C-MTP38, a Novel PET Ligand for Phosphodiesterase 7
https://repo.qst.go.jp/records/81802
https://repo.qst.go.jp/records/818028e111af2-56e9-46fb-bc85-85e704efbd87
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2021-02-09 | |||||
| タイトル | ||||||
| タイトル | A First-in-human Study of 11C-MTP38, a Novel PET Ligand for Phosphodiesterase 7 | |||||
| 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 |
Manabu, Kubota
× Manabu, Kubota× Chie, Seki× Yasuyuki, Kimura× Keisuke, Takahata× Hitoshi, Shimada× Yuhei, Takado× Kiwamu, Matsuoka× Kenji, Tagai× Yasunori, Sano× Yamamoto, Yasuharu× Maki, Okada× Tatsuya, Kikuchi× Masanori, Ichise× Kazunori, Kawamura× Zhang, Ming-Rong× Makoto, Higuchi× Manabu, Kubota× Chie, Seki× Yasuyuki, Kimura× Keisuke, Takahata× Hitoshi, Shimada× Yuhei, Takado× Kiwamu, Matsuoka× Kenji, Tagai× Yasunori, Sano× Yamamoto, Yasuharu× Maki, Okada× Tatsuya, Kikuchi× Masanori, Ichise× Kazunori, Kawamura× Zhang, Ming-Rong× Makoto, Higuchi |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Purpose: Phosphodiesterase 7 (PDE7) is an enzyme that selectively hydrolyses cyclic adenosine monophosphate, and its dysfunction is implicated in neuropsychiatric diseases. However, in vivo visualization of PDE7 in human brains has hitherto not been possible. Using the novel PET ligand 11C-MTP38, which we recently developed, we aimed to image and quantify PDE7 in living human brains. Methods: Seven healthy males underwent a 90-min PET scan after injection of 11C-MTP38. We performed arterial blood sampling and metabolite analysis of plasma in six subjects to obtain a metabolite-corrected input function. Regional total distribution volumes (VT’s) were estimated using compartment models, and Logan plot and Ichise multilinear analysis (MA1). We further quantified the specific radioligand binding using the original multilinear reference tissue model (MRTMO) and standardized uptake value ratio (SUVR) method with the cerebellar cortex as reference. Results: PET images with 11C-MTP38 showed relatively high retentions in several brain regions, including in the striatum, globus pallidus, and thalamus, as well as fast washout from the cerebellar cortex, in agreement with the known distribution of PDE7. VT values were robustly estimated by two-tissue compartment model analysis (mean VT = 4.2 for the pallidum), Logan plot, and MA1, all in excellent agreement with each other, suggesting the reversibility of 11C-MTP38 binding. Furthermore, there were good agreements between binding values estimated by indirect method and those estimated by both MRTMO and SUVR, indicating that these methods could be useful for reliable quantification of PDE7. Because MRTMO and SUVR do not require arterial blood sampling, they are the most practical for the clinical use of 11C-MTP38-PET. Conclusion: We have provided the first demonstration of PET visualization of PDE7 in human |
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| 書誌情報 |
European Journal of Nuclear Medicine and Molecular Imaging 巻 48, 号 9, p. 2846-2855, 発行日 2021-02 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 1619-7070 | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 33566152 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1007/s00259-021-05235-0 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://link.springer.com/article/10.1007/s00259-021-05235-0 | |||||
