| アイテムタイプ |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2026-01-09 |
| タイトル |
|
|
タイトル |
Radiosynthesis and Preclinical Evaluation of a Novel 11C‑Labeled Pyrazolopyrimidine Derivative for Positron Emission Tomography Imaging of Phosphodiesterase 2A |
|
言語 |
en |
| 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 |
| 著者 |
Yinlong Li
Mori Wakana
Zhendong Song
Yamasaki Tomoteru
Taoqian Zhao
Jiahui Chen
Yiding Zhang
Xin Zhou
Xie Lin
Tomomi Kokufuta
Kuan Hu
Qilong Hu
Fujinaga Masayuki
Xiaoyan Li
Kumata Katsushi
Chongjiao Li
Zhenkun Sun
Yabiao Gao
Danielle E. Hoyle
Jimmy S. Patel
Hongjie Yuan
Zhang Ming-Rong
Steven H. Liang
|
| 抄録 |
|
|
内容記述タイプ |
Abstract |
|
内容記述 |
Phosphodiesterase 2A (PDE2A) plays a vital role in regulating cyclic nucleotide signaling by hydrolyzing cAMP and cGMP in the central nervous system (CNS). This enzymatic activity is essential for neuronal function, and PDE2A has emerged as a molecular target for neuroimaging in neuropsychiatric disorders and neurodegenerative diseases. In this study, we evaluated the novel 11C-labeled positron emission tomography (PET) radioligand [11C]1 derived from a pyrazolopyrimidine-based PDE2A inhibitor. The radiosynthesis of [11C]1 was accomplished via [11C]methyl iodide-mediated methylation of precursor 9 under mild conditions, yielding [11C]1 with high purity (99%) and high molar activity (154 ± 66 GBq/μmol). In vitro autoradiography demonstrated high radiotracer accumulation in regions with abundant PDE2A expression, including the striatum and substantia nigra. However, dynamic PET imaging in rats showed a relatively uniform distribution throughout the brain and no significant blocking effects. Further optimization in medicinal chemistry is necessary to improve the in vivo performance of the pyrazolopyrimidine-based PDE2A tracer scaffold. |
| 書誌情報 |
ACS Medicinal Chemistry Letters
発行日 2025-12
|
| 出版者 |
|
|
出版者 |
American Chemical Society |
| ISSN |
|
|
収録物識別子タイプ |
ISSN |
|
収録物識別子 |
1948-5875 |
| DOI |
|
|
|
識別子タイプ |
DOI |
|
|
関連識別子 |
10.1021/acsmedchemlett.5c00649 |
