Development of PET probes for gama 8-dependent transmembrane AMPA receptor regulatory protein

• Project/Area Number: 20H03635
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Single-year Grants
• Section: 一般
• Review Section: Basic Section 52040:Radiological sciences-related
• Research Institution: National Institutes for Quantum Science and Technology
• Principal Investigator: 張 明栄 国立研究開発法人量子科学技術研究開発機構, 量子医科学研究所 先進核医学基盤研究部, 部長 (80443076)
• Co-Investigator(Kenkyū-buntansha): 胡 寛 国立研究開発法人量子科学技術研究開発機構, 量子医科学研究所 先進核医学基盤研究部, 研究員 (00827678) ; 謝 琳 国立研究開発法人量子科学技術研究開発機構, 量子医科学研究所 先進核医学基盤研究部, 主任研究員 (30623558) ; 河村 和紀 国立研究開発法人量子科学技術研究開発機構, 量子医科学研究所 先進核医学基盤研究部, グループリーダー (50401766) ; 藤永 雅之 国立研究開発法人量子科学技術研究開発機構, 量子医科学研究所 先進核医学基盤研究部, 主任研究員 (70623726) ; 山崎 友照 国立研究開発法人量子科学技術研究開発機構, 量子医科学研究所 先進核医学基盤研究部, 主任研究員 (80627563)
• Project Period (FY): 2020-04-01 – 2024-03-31
• Project Status: Completed (Fiscal Year 2022)
• Budget Amount: ¥17,420,000 (Direct Cost: ¥13,400,000、Indirect Cost: ¥4,020,000); Fiscal Year 2022: ¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000); Fiscal Year 2021: ¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000); Fiscal Year 2020: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
• Keywords: AMPA受容体 / 膜貫通AMPA受容体調節性タンパク質-γ8 / TARP-γ8 / [11C]TARP-2105 / PET / オートラジオグラフィ / オートラジオグラフィー / 膜貫通AMPA受容体調節性タンパク質

Outline of Research at the Start

本申請課題はAMPA受容体の補助サブユニットTARP-γ8を画像化できる、臨床有用なPETプローブを開発することを目的とする。事前の予備実験で得たPETプローブ候補をベースをして、計算化学などの手法により数十種の新規化合物を設計し、合成する。これらの化合物がTARP-γ8との結合特性を調べ、有望な化合物候補に対し、11Cや18Fによるプローブ化を行う。標識された放射性化合物に対し、マウス、ラットなどを用いて、解剖法、インビトロオートラジオグラフィ及びPETなどを用いて、これらの有用性と安全性/毒性を評価する。また、有望なPETプローブに対し、First-in-Human研究を目指す。

Outline of Annual Research Achievements

申請者らはAMPA受容体の陽電子断層撮像法(PET)用分子プローブを開発している。現在までAMPA本体サブユニットを標的とするPETプローブを開発し、臨床PET研究を行なってきた。今回の研究課題は、AMPA補助サブユニットの一つであるTARP-γ8を標的とするPETプローブを創出することを目的とした。
今年度申請者らは、前年度設計した化合物の化学合成を継続して行なった。合成した化合物の中から、TARP-γ8に対して高い活性と選択性を有する8種の新規誘導体を見出した。その中から、適切な親和性、選択性及び物理化学性質を有する２種の化合物TARP-2103及び TARP-2105を選び、[11C]CH3Iによる標識を行い、自動合成装置にて[11C]TARP-2103及び [11C]TARP-2105を合成した。これらのPETプローブを用い、マウスやラットを用いたPETイメージング、解剖法による放射能分布試験、ラットオートラジオグラフィ、及び代謝物分析を行い、PETプローブとしての有用性を評価した。
その結果、[11C]TARP-2105はマウス、ラットへの脳移行性が比較的よく、インビトロARGでは、TARP-γ8が高い海馬などの領域において、高い特異結合を示した。また、PETでは本プローブはラット脳内において、海馬に対して比較的高い特異結合と選択性を示した。一方、ラット脳内において、放射性代謝物が少なく、未変化体はほとんどであった。さらに、[11C]TARP-2105を使い、PETによる各種の定量方法を詳細に検討し、比較を行ったことにより、生きたラット脳におけるTARP-γ8を定量することができた。これらの結果から、 [11C]TARP-2105は世界初のPETプローブ候補として、ヒト脳内におけるTARP-γ8の画像化及び機能解明に役立つことが期待できた。

Research Progress Status

令和4年度が最終年度であるため、記入しない。

Strategy for Future Research Activity

令和4年度が最終年度であるため、記入しない。

Research Products

• [Int'l Joint Research] MGH/Emory University/The Scripps Research Institute(米国)
• [Int'l Joint Research] Nanjing Medical University/Chinese Academy of Medical Sciences/Jinan University(中国)
• [Int'l Joint Research] University of Zurich(スイス)
• [Journal Article] Small-animal PET study for noninvasive quantification of transmembrane AMPA receptor regulatory protein γ8 (TARP γ-8) in the brain (2023)
  • Author(s): Yamasaki Tomoteru、Ishii Hideki、Hiraishi Atsuto、Kumata Katsushi、Wakizaka Hidekatsu、Zhang Yiding、Kurihara Yusuke、Ogawa Masanao、Nengaki Nobuki、Chen Jiahui、Li Yinlong、Liang Steven、Zhang Ming-Rong
  • Journal Title: Journal of Cerebral Blood Flow and Metabolism Volume: 43 Issue: 6 Pages: 893-904
  • DOI: 10.1177/0271678x231152025
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Development of a 68Gallium-Labeled D-Peptide PET Tracer for Imaging Programmed Death-Ligand 1 Expression (2023)
  • Author(s): Zhang Lulu、Zhang Siqi、Wu Wenyu、Wang Xingkai、Shen Jieting、Wang Dongyuan、Hu Kuan、Zhang Ming-Rong、Wang Feng、Wang Rui
  • Journal Title: Journal of Visualized Experiments Volume: 4 Issue: 192
  • DOI: 10.3791/65047
  • Peer Reviewed / Open Access / Int'l Joint Research
• [Journal Article] A 211At-labelled mGluR1 inhibitor induces cancer senescence to elicit long-lasting anti-tumor efficacy (2023)
  • Author(s): Xie Lin、Zhang Lulu、Hu Kuan、Hanyu Masayuki、Zhang Yiding、Fujinaga Masayuki、Minegishi Katsuyuki、Ohkubo Takayuki、Nagatsu Kotaro、Jiang Cuiping、Shimokawa Takashi、Ashisuke Kazuma、Okonogi Noriyuki、Yamada Shigeru、Wang Feng、Wang Rui、Zhang Ming-Rong
  • Journal Title: Cell Reports Medicine Volume: 4 Issue: 4 Pages: 100960-100960
  • DOI: 10.1016/j.xcrm.2023.100960
  • Peer Reviewed / Open Access / Int'l Joint Research
• [Journal Article] Imaging of Transmembrane AMPA Receptor Regulatory Proteins by Positron Emission Tomography (2022)
  • Author(s): Yu Qingzhen、Kumata Katsushi、Rong Jian、Chen Zhen、Yamasaki Tomoteru、Chen Jiahui、Xiao Zhiwei、Ishii Hideki、Hiraishi Atsuto、Shao Tuo、Zhang Yiding、Hu Kuan、Xie Lin、Fujinaga Masayuki、Zhao Chunyu、Mori Wakana、Collier Thomas、Haider Ahmed、Tomita Susumu、Zhang Ming-Rong、Liang Steven
  • Journal Title: Journal of Medicinal Chemistry Volume: 65 Issue: 13 Pages: 9144-9158
  • DOI: 10.1021/acs.jmedchem.2c00377
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Scandium Triflate-Catalyzed N-[18F]Fluoroalkylation of Aryl- Or Heteroaryl-Amines with [18F]Epifluorohydrin under Mild Conditions (2022)
  • Author(s): Fujinaga Masayuki、Ohkubo Takayuki、Yamasaki Tomoteru、Kumata Katsushi、Nengaki Nobuki、Zhang Ming-Rong
  • Journal Title: Organic Letters Volume: 24 Issue: 22 Pages: 4024-4028
  • DOI: 10.1021/acs.orglett.2c01459
  • Peer Reviewed
• [Journal Article] A novel monoacylglycerol lipase-targeted 18F-labeled probe for positron emission tomography imaging of brown adipose tissue in the energy network (2022)
  • Author(s): Cheng Ran、Fujinaga Masayuki、Yang Jing、Zhang Ming-Rong、Liang Steven et al
  • Journal Title: Acta Pharmacologica Sinica Volume: 43 Issue: 11 Pages: 3002-3010
  • DOI: 10.1038/s41401-022-00912-8
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Rapid ‘on-column’ preparation of hydrogen [11C]cyanide from [11C]methyl iodide via [11C]formaldehyde (2022)
  • Author(s): Tatsuya Kikuchi, Masanao Ogawa, Toshimitsu Okamura, Antony D. Gee, Ming-Rong Zhang
  • Journal Title: Chemical Science Volume: 13 Issue: 12 Pages: 3556-3562
  • DOI: 10.1039/d1sc07033a
  • Peer Reviewed / Open Access / Int'l Joint Research
• [Journal Article] 11C-Labeled Radiotracer for Noninvasive and Quantitative Assessment of the Thiocyanate Efflux System in the Brain (2022)
  • Author(s): Okamura Toshimitsu、Tsukamoto Satoshi、Okada Maki、Kikuchi Tatsuya、Aizawa Ryutaro、Wakizaka Hidekatsu、Nengaki Nobuki、Ogawa Masanao、Ishii Hideki、Zhang Ming-Rong
  • Journal Title: Bioconjugate Chemistry Volume: 33 Issue: 9 Pages: 1654-1662
  • DOI: 10.1021/acs.bioconjchem.2c00277
  • Peer Reviewed
• [Journal Article] Synthesis of [11C]carbonyl-labeled cyclohexyl (5-(2-acetamidobenzo[d]thiazol-6-yl)-2-methylpyridin-3-yl)carbamate ([11C-carbonyl]PK68) as a potential PET tracer for receptor-interacting protein 1 kinase (2022)
  • Author(s): Yamasaki Tomoteru、Kumata Katsushi、Hiraishi Atsuto、Zhang Yiding、Wakizaka Hidekatsu、Kurihara Yusuke、Nengaki Nobuki、Zhang Ming-Rong
  • Journal Title: EJNMMI Radiopharmacy and Chemistry Volume: 7 Issue: 1 Pages: 1-7
  • DOI: 10.1186/s41181-022-00156-1
  • Peer Reviewed / Open Access
• [Journal Article] Assessment of cholesterol homeostasis in the living human brain (2022)
  • Author(s): Haider Ahmed、Zhao Chunyu、Wang Lu、Zhang Ming-Rong、Liang Steven et al
  • Journal Title: Science Translational Medicine Volume: 14 Issue: 665
  • DOI: 10.1126/scitranslmed.adc9967
  • Peer Reviewed / Open Access / Int'l Joint Research
• [Journal Article] Upregulation of striatal metabotropic glutamate receptor subtype 1 (mGluR1) in rats with excessive glutamate release induced by N-acetylcysteine (2022)
  • Author(s): Yamasaki Tomoteru, Okada Maki, Hiraishi Atsuto, Mori Wakana, Zhang Yiding, Fujinaga Masayuki, Wakizaka Hidekatsu, Kurihara Yusuke, Nengaki Nobuki, Zhang Ming-Rong
  • Journal Title: Neurotoxicity Research Volume: 40 Issue: 1 Pages: 26-35
  • DOI: 10.1007/s12640-021-00449-4
  • Peer Reviewed
• [Journal Article] Automated radiosynthesis of [11C]MTP38-a phosphodiesterase 7 imaging tracer using [11C]hydrogen cyanide for clinical applications (2022)
  • Author(s): Kawamura Kazunori、Hashimoto Hiroki、Ohkubo Takayuki、Hanyu Masayuki、Ogawa Masanao、Nengaki Nobuki、Arashi Daisuke、Kurihara Yusuke、Fujishiro Tomoya、Togashi Takahiro、Sakai Toshiyuki、Muto Masatoshi、Takei Makoto、Ishii Hideki、Saijo Takeaki、Matsumura Takehiko、Obokata Naoyuki、Zhang Ming‐Rong
  • Journal Title: Journal of Labelled Compounds and Radiopharmaceuticals Volume: 65 Issue: 5 Pages: 140-146
  • DOI: 10.1002/jlcr.3965
  • Peer Reviewed
• [Journal Article] Whole-body PET tracking of a D-dodecapeptide and its radiotheranostic potential for PD-L1 overexpressing tumors (2022)
  • Author(s): Hu Kuan, Wu Wenyu, Xie Lin, Geng Hao, Zhang Yiding, Hanyu Masayuki, Zhang Lulu, Liu Yinghuan, Nagatsu Kotaro, Suzuki Hisashi, Guo Jialin, Wu Yundong, Li Zigang, Wang Feng, Zhang Ming-Rong
  • Journal Title: Acta Pharmaceutica Sinica B Volume: 12 Issue: 3 Pages: 1363-1376
  • DOI: 10.1016/j.apsb.2021.09.016
  • Peer Reviewed / Open Access / Int'l Joint Research
• [Journal Article] Neuroprotective effects of minocycline and KML29, a potent inhibitor of monoacylglycerol lipase, in an experimental stroke model: a small-animal positron emission tomography study (2021)
  • Author(s): Yamasaki Tomoteru, Hatori Akiko, Zhang Yiding, Kurihara Yusuke, Ogawa Masanao, Wakizaka Hidekatsu, Rong Jian, Wang Lu, Huan Liang, Zhang Ming-Rong
  • Journal Title: Theranostics Volume: 11 Issue: 19 Pages: 9492-9502
  • DOI: 10.7150/thno.64320
  • Peer Reviewed / Open Access / Int'l Joint Research
• [Journal Article] Design, Synthesis, and Evaluation of 11C-Labeled 3-Acetylindole Derivatives as Novel Positron-Emission Tomography Imaging Agent for Diacylglycerol Kinase Gamma (DGKγ) in Brain (2021)
  • Author(s): Hattori Yasushi, Yamasaki Tomoteru, Ohashi Tomohiro, Miyanohana Yuhei, Kusumoto Tomokazu, Maeda Ryouta, Miyamoto Maki, Debori Yasuyuki, Hata Akito, Zhang Yiding, Wakizaka Hidekatsu, Wakabayashi Takeshi, Fujinaga Masayuki, Yamashita Ryo, Zhang Ming-Rong, Koike Tatsuki
  • Journal Title: Journal of Medicinal Chemistry Volume: 64 Issue: 16 Pages: 11990-12002
  • DOI: 10.1021/acs.jmedchem.1c00584
  • Peer Reviewed
• [Journal Article] Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold (2021)
  • Author(s): Rong Jian, Mori Wakana, Xia Xiaotian, Zhang Ming-Rong, Liang Steven
  • Journal Title: Journal of Medicinal Chemistry Volume: 64 Issue: 19 Pages: 14283-14298
  • DOI: 10.1021/acs.jmedchem.1c00747
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Imaging the trace amine-associated receptor 1 by positron emission tomography (2021)
  • Author(s): Sun Jiyun, Chen Jiahui, Kumata Katsushi, Xiao Zhiwei, Rong Jiang, Haider Ahmed, Shao Tuo, Wang Lu, Xu Hao, Zhang Ming-Rong, Liang Steven
  • Journal Title: Tetrahedron Letters Volume: 70 Pages: 153007-153007
  • DOI: 10.1016/j.tetlet.2021.153007
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Automated radiosynthesis of two 18F-labeled tracers containing 3-fluoro-2-hydroxypropyl moiety, [18F]FMISO and [18F]PM-PBB3, via [18F]epifluorohydrin (2021)
  • Author(s): Ohkubo Takayuki、Kurihara Yusuke、Ogawa Masanao、Nengaki Nobuki、Fujinaga Masayuki、Mori Wakana、Kumata Katsushi、Hanyu Masayuki、Furutsuka Kenji、Hashimoto Hiroki、Kawamura Kazunori、Zhang Ming-Rong
  • Journal Title: EJNMMI Radiopharmacy and Chemistry Volume: 6 Issue: 1 Pages: 23-23
  • DOI: 10.1186/s41181-021-00138-9
  • Peer Reviewed / Open Access
• [Journal Article] Off-tumor IDO1 target engagements determine the cancer-immune set point and predict the immunotherapeutic efficacy (2021)
  • Author(s): Xie Lin, Hu Kuan, Duo Yanhong, Shimokawa Takashi, Kumata Katsushi, Zhang Yiding, Jiang Cuiping, Zhang Lulu, Nengaki Nobuki, Wakizaka Hidekatsu, Cao Yihai, Zhang Ming-Rong
  • Journal Title: Journal for ImmunoTherapy of Cancer Volume: 9 Issue: 6 Pages: e002616-e002616
  • DOI: 10.1136/jitc-2021-002616
  • Peer Reviewed / Open Access / Int'l Joint Research
• [Journal Article] Development of a highly-specific 18F-labeled irreversible positron emission tomography tracer for monoacylglycerol lipase mapping (2021)
  • Author(s): Chen Zhen, Wakana Mori, Rong Jian, Schafroth Michael A, Ogasawara Daisuke, Yamasaki Tomoteru, Hiraishi Atsuto, Hatori Akiko, Zhang Yiding, Hu Kuan, Fujinaga Masayuki, Cravatt Benjamin F., Josephson Lee, Zhang Ming-Rong, Liang Steven
  • Journal Title: Acta Pharmaceutica Sinica B Volume: 11 Pages: 1686-1695
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Identification and Development of a New Positron Emission Tomography Ligand 4-(2-Fluoro-4-[11C]methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide for Imaging Metabotropic Glutamate Receptor Subtype 2 (mGlu2) (2020)
  • Author(s): Yamasaki Tomoteru、Zhang Xiaofei、Kumata Katsushi、Zhang Yiding、Deng Xiaoyun、Fujinaga Masayuki、Chen Zhen、Mori Wakana、Hu Kuan、Wakizaka Hidekatsu、Hatori Akiko、Xie Lin、Ogawa Masanao、Nengaki Nobuki、Van Richard、Shao Yihan、Sheffler Douglas J.、Cosford Nicholas D. P.、Liang Steven H.、Zhang Ming-Rong
  • Journal Title: Journal of Medicinal Chemistry Volume: 63 Issue: 20 Pages: 11469-11483
  • DOI: 10.1021/acs.jmedchem.9b01991
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] 3-(Cyclopropylmethyl)-7-((4-(4-[11C]methoxyphenyl)piperidin-1-yl)methyl)-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine: Synthesis and preliminary evaluation for PET imaging of metabotropic glutamate receptor subtype 2 (2020)
  • Author(s): Kumata Katsushi、Zhang Yiding、Ogawa Masanao、Kurihara Yusuke、Mori Wakana、Hu Kuan、Fujinaga Masayuki、Nengaki Nobuki、Zhang Ming-Rong
  • Journal Title: Bioorganic & Medicinal Chemistry Letters Volume: 30 Issue: 23 Pages: 127555-127555
  • DOI: 10.1016/j.bmcl.2020.127555
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Synthesis and preliminary studies of 11C-labeled tetrahydro-1,7-naphthyridine-2-carboxamides for PET imaging of metabotropic glutamate receptor 2 (2020)
  • Author(s): Zhang Xiaofei、Zhang Yiding、Chen Zhen、Shao Tuo、Van Richard、Kumata Katsushi、Deng Xiaoyun、Fu Hualong、Yamasaki Tomoteru、Rong Jian、Hu Kuan、Hatori Akiko、Xie Lin、Yu Qingzhen、Ye Weijian、Xu Hao、Sheffler Douglas J.、Cosford Nicholas D. P.、Shao Yihan、Tang Pingping、Wang Lu、Zhang Ming-Rong、Liang Steven H.
  • Journal Title: Theranostics Volume: 10 Issue: 24 Pages: 11178-11196
  • DOI: 10.7150/thno.42587
  • Peer Reviewed / Open Access / Int'l Joint Research
• [Journal Article] Synthesis and preliminary evaluation of novel 11C-labeled GluN2B-selective NMDA receptor negative allosteric modulators (2020)
  • Author(s): Sun Ji-yun、Kumata Katsushi、Chen Zhen、Zhang Yi-ding、Chen Jia-hui、Hatori Akiko、Fu Hua-long、Rong Jian、Deng Xiao-yun、Yamasaki Tomoteru、Xie Lin、Hu Kuan、Fujinaga Masayuki、Yu Qing-zhen、Shao Tuo、Collier Thomas Lee、Josephson Lee、Shao Yi-han、Du Yun-fei、Wang Lu、Xu Hao、Zhang Ming-rong、Liang Steven H
  • Journal Title: Acta Pharmacologica Sinica Volume: 42 Issue: 3 Pages: 491-498
  • DOI: 10.1038/s41401-020-0456-9
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Synthesis and preliminary evaluation of 4-hydroxy-6-(3-[11C]methoxyphenethyl)pyridazin-3(2H)-one, a 11C-labeled -amino acid oxidase (DAAO) inhibitor for PET imaging (2020)
  • Author(s): Deng Xiaoyun、Zhang Yiding、Chen Zhen、Kumata Katsushi、Van Richard、Rong Jian、Shao Tuo、Hatori Akiko、Mori Wakana、Yu Qingzhen、Hu Kuan、Fujinaga Masayuki、Wey Hsiao-Ying、Shao Yihan、Josephson Lee、Murtas Giulia、Pollegioni Loredano、Zhang Ming-Rong、Liang Steven
  • Journal Title: Bioorganic & Medicinal Chemistry Letters Volume: 30 Issue: 16 Pages: 127326-127326
  • DOI: 10.1016/j.bmcl.2020.127326
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Radiosynthesis and evaluation of 4-(6-[18F]Fluoro-4-(5-isopropoxy-1H-indazol-3-yl)pyridin-2-yl)morpholine as a novel radiotracer candidate targeting leucine-rich repeat kinase 2 (2020)
  • Author(s): Mori Wakana、Yamasaki Tomoteru、Hattori Yasushi、Zhang Yiding、Kumata Katsushi、Fujinaga Masayuki、Hanyu Masayuki、Nengaki Nobuki、Zhang Hong、Zhang Ming-Rong
  • Journal Title: RSC Medicinal Chemistry Volume: 11 Issue: 6 Pages: 676-684
  • DOI: 10.1039/c9md00590k
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Development of an In Vivo Method to Estimate Effective Drug Doses and Quantify Fatty Acid Amide Hydrolase in Rodent Brain using Positron Emission Tomography Tracer N-(3,4-dimethylisoxazol-5-yl)piperazine-4-[4-(2-fluoro-4-[11C]methylphenyl)thiazol-2-yl]-1-carboxamide ([11C]DFMC) (2020)
  • Author(s): Yamasaki Tomoteru、Ohya Tomoyuki、Mori Wakana、Zhang Yiding、Wakizaka Hidekatsu、Nengaki Nobuki、Fujinaga Masayuki、Kikuchi Tatsuya、Zhang Ming-Rong
  • Journal Title: Journal of Pharmacology and Experimental Therapeutics Volume: - Issue: 3 Pages: 353-360
  • DOI: 10.1124/jpet.119.263772
  • Peer Reviewed
• [Journal Article] Synthesis and evaluation of 6-(11C-methyl(4-(pyridin-2-yl)thiazol-2-yl)amino)benzo[d]thiazol-2(3H)-one for imaging γ-8 dependent transmembrane AMPA receptor regulatory protein by PET (2020)
  • Author(s): Yu Qingzhen、Kumata Katsushi、Li Hua、Zhang Yiding、Chen Zhen、Zhang Xiaofei、Shao Tuo、Hatori Akiko、Yamasaki Tomoteru、Xie Lin、Hu Kuan、Wang Gangqiang、Josephson Lee、Sun Shaofa、Zhang Ming-Rong、Liang Steven H.
  • Journal Title: Bioorganic & Medicinal Chemistry Letters Volume: 30 Issue: 4 Pages: 126879-126879
  • DOI: 10.1016/j.bmcl.2019.126879
  • Peer Reviewed / Int'l Joint Research
• [Presentation] A Platform for Radiopharmaceuticals Development and Production (2023)
  • Author(s): Zhang Ming-Rong
  • Organizer: Molecular Imaging Forum
  • Int'l Joint Research / Invited
• [Presentation] Innovation of Radiopharmaceuticals from PET to TRT (2023)
  • Author(s): Zhang Ming-Rong
  • Organizer: Nuclear Technology Application Development Forum
  • Int'l Joint Research / Invited
• [Presentation] Synthesis and evaluation of PET ligands for monoacylglycerol lipase in brain (2022)
  • Author(s): Mori Wakana, Yusuke Kurihara, Yamasaki Tomoteru, Hatori Akiko, Yiding Zhang, Fujinaga Masayuki, Zhang Ming-Rong
  • Organizer: iSRS (International Symposium on Radiopharmaceutical Sciences)
  • Int'l Joint Research
• [Presentation] Radiosynthesis of 6-(2-cyclobutyl-5-(methyl-11C)-3H-imidazo[4,5-b]pyridin-3-yl)benzo[d]thiazol-2(3H)-one and (2-cyclobutyl-3-(1H-indazol-5-yl)-5-[11C]methyl-3H-imidazo[4,5-b]pyridine for imaging γ-8 dependent transmembrane AMPA receptor regulatory protein (2022)
  • Author(s): Qingzhen Yu, Kumata Katsushi, Thomas Lee Collier, Susumu Tomita, Zhang Ming-Rong, Steven Liang
  • Organizer: iSRS (International Symposium on Radiopharmaceutical Sciences)
  • Int'l Joint Research
• [Presentation] The fully-automated synthesis of [11C]CF3-aryl derivatives with [11C]fluoroform (2022)
  • Author(s): Fujinaga Masayuki, Ogawa Masanao, Nengaki Nobuki, Kumata Katsushi, Mori Wakana, Zhang Ming-Rong
  • Organizer: iSRS (International Symposium on Radiopharmaceutical Sciences)
  • Int'l Joint Research
• [Presentation] Development of [18F]FHP-TMP as a PET gene reporter tracer for imaging of E.coli dihydrofolate reductase in the mammalian brain (2022)
  • Author(s): Takayuki Ohkubo, Shimojo Masafumi, Ono Maiko, Fujinaga Masayuki, Ogawa Masanao, Nengaki Nobuki, Nagai Yuji, Minamimoto Takafumi, Higuchi Makoto, Zhang Ming-Rong
  • Organizer: iSRS (International Symposium on Radiopharmaceutical Sciences)
  • Int'l Joint Research
• [Presentation] Radiolabeling and evaluation of cyclohexyl (5-(2-acetamidobenzo[d]thiazol-6-yl)-2-methylpyridin-3-yl) carbamate (PK68), a potent inhibitor for receptor interacting protein 1 kinase (RIP1) (2022)
  • Author(s): Kumata Katsushi, Yamasaki Tomoteru, Hiraishi Atsuto, Yiding Zhang, Wakizaka Hidekatsu, Ogawa Masanao, Nengaki Nobuki, Zhang Ming-Rong
  • Organizer: iSRS (International Symposium on Radiopharmaceutical Sciences)
  • Int'l Joint Research
• [Presentation] Recent Advances on Radiopharmaceuticals in Brain PET Imaging and Targeted Radionuclide Therapy (2022)
  • Author(s): Zhang Ming-Rong
  • Organizer: Global Distinguished Scientists Forum on Molecular Imaging, Molecular Medicine and Pharmacology
  • Int'l Joint Research / Invited
• [Presentation] Standard Production and Quality Control of PET Drugs in Japan (2022)
  • Author(s): Zhang Ming-Rong
  • Organizer: Forum on Nuclear Medicine and Quality Control in China
  • Int'l Joint Research / Invited
• [Presentation] 免疫チェックポイントPETプローが免疫治療への応用現状と展望 (2022)
  • Author(s): Zhang Ming-Rong
  • Organizer: 中国核学会核医学分科会/遼寧省核学会定期会議
  • Int'l Joint Research / Invited
• [Presentation] Development of a novel PET tracer for imaging of γ-8 dependent transmembrane AMPA receptor regulatory protein (2021)
  • Author(s): Yu Qingzhen, Liang Steven, Zhang Ming-Rong
  • Organizer: eSRS, Society of Radiopharmaceutical Sciences
  • Int'l Joint Research
• [Presentation] Synthesis, Radiolabeling and Biological Evaluation of a Novel Trace Amine-Associated Receptor 1 (TAAR1) PET radioligand (2021)
  • Author(s): Haider Ahmed, Sun Jiyun, Chen Jiahui, Rong Jian, Shao Tuo, Wang Lu, Xu Hao, Zhang Ming-Rong, Liang Steven
  • Organizer: eSRS, Society of Radiopharmaceutical Sciences
  • Int'l Joint Research
• [Presentation] 認知症PETプローブ開発と応用 (2021)
  • Author(s): Zhang Ming-Rong
  • Organizer: 17th Nuclear Medicine Academic Conference of Jiangsu Medical Association
  • Int'l Joint Research / Invited
• [Presentation] Development and Production of Radiopharmaceuticals in National Institutes for Quantum and Radiological Science and Technology (QST) (2021)
  • Author(s): Zhang Ming-Rong
  • Organizer: PETセミナー in Yale University
  • Int'l Joint Research / Invited
• [Presentation] Radiolabeling agents for development of novel PET tracers for neuroimaging (2021)
  • Author(s): Zhang Ming-Rong
  • Organizer: The 7th PET/CT-MRI Multimodal Molecular Imaging Summit Forum, The 3rd International symposium on PET Ligand Developmen
  • Int'l Joint Research / Invited
• [Presentation] PETプローブの開発と臨床応用 (2021)
  • Author(s): 張 明栄
  • Organizer: 順天堂大学大学院医学研究科循環器内科 循環器セミナー
  • Invited
• [Presentation] Whole-body PET Tracking of a D-dodecapeptide and its Radiotheranostic Potential for PD-L1 overexpressed tumors (2021)
  • Author(s): Hu Kuan, Xie Lin, Zhang Yiding, Hanyu Masayuki, Zhang Ming-Rong
  • Organizer: SNMMI2021, Society of Nuclear Medicine and Molecular Imaging
  • Int'l Joint Research
• [Presentation] Design, Synthesis, and Evaluation of 11C-Labeled 3-Acetyl-indole Derivatives as Novel Positron-Emission Tomography Imaging Agent for Diacylglycerol Kinase Gamma (DGKγ) in Brain (2021)
  • Author(s): Hattori Yasushi, Tomoteru Yamasaki, Ohashi Tomohiro, Miyanohana Yuhei, Kusumoto Tomokazu, Maeda Ryouta, Miyamoto Maki, Debori Yasuyuki, Hata Akiko, Zhang Yiding, Wakizaka Hidekatsu, Wakabayashi Takeshi, Fujinaga Masayuki, Yamashita Ryo, Zhang Ming-Rong, Koike Tatsuki
  • Organizer: AIMECS 2021, Asian Federation for Medicinal Chemistry
  • Int'l Joint Research
• [Presentation] PET imaging of PD-L1 overexpressing tumors with a 68Ga labeled D-dodecapeptide (2021)
  • Author(s): Hu Kuan, Xie Lin, Hanyu Masayuki, Zhang Yiding, Zhang Ming-Rong
  • Organizer: eSRS, Society of Radiopharmaceutical Sciences
  • Int'l Joint Research
• [Presentation] Imaging urokinase plasminogen activator with a cyclic peptide-based PET tracer (2021)
  • Author(s): Hu Kuan, Xie Lin, Zhang Yiding, Hanyu Masayuki, Zhang Ming-Rong
  • Organizer: 第61回日本核医学会学術総会, 日本核医学会
• [Presentation] Preclinical evaluation of radiolabeled negative allosteric modulators for PET imaging of metabotropic glutamate receptor 2 (2020)
  • Author(s): Wang Lu, Xiaofei Zhang, Zhen Chen, Hao Xu, Yihan Shao, Douglas Sheffler, Ming-Rong Zhang, Steven H. Liang
  • Organizer: SNMMI 2020 Annual Meeting
  • Int'l Joint Research
• [Presentation] Synthesis and preclinical evaluation of 11C-labeled (6-aryl-1H-pyrrolo[3,2-b]pyridin-1-yl)acetamide for imaging GluN2B subunit of NMDA receptors (2020)
  • Author(s): Jiyun Sun, Zhen Chen, Jiahui Chen, Hualong Fu, Tuo Shao, Wang Lu, Hao Xu, Ming-Rong Zhang, Steven H. Liang
  • Organizer: SNMMI 2020 Annual Meeting
  • Int'l Joint Research
• [Presentation] 脳内D－アミノ酸オキシダーゼの新規PETプローブ[11C]DAO-1903の合成と評価 (2020)
  • Author(s): 張 一鼎, 熊田 勝志, 小川 政直, 栗原 雄祐, 念垣 信樹, 張 明栄
  • Organizer: 第60回日本核医学会学術総会
• [Presentation] 脳内NMDA受容体を標的としたPET薬剤の合成と評価 (2020)
  • Author(s): 熊田 勝志, 張 一鼎, 山崎 友照, 念垣 信樹, 張 明栄
  • Organizer: 第60回日本核医学会学術総会
• [Presentation] グルタミン酸受容体サブタイプ特異的なPETプローブの開発 (2020)
  • Author(s): 張 明栄
  • Organizer: 第60回日本核医学会学術総会
  • Invited
• [Book] Positron Emission Tomography (PET) Imaging of Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Based on a Negative Allosteric Modulator Radioligand. (2021)
  • Author(s): Xiaofei Zhang, Zhiwei Xiao, Kumata Katsushi, Yamasaki Tomoteru, Lee Josephson, Zhang Ming-Rong, Wang Lu, Steven H. Liang
  • Total Pages: 314
  • Publisher: Humana, New York, NY
  • ISBN: 9781071611074
• [Book] Attempts to Image MRP1 Function in the Blood-Brain Barrier Using the Metabolite Extrusion Method (2020)
  • Author(s): Toshimitsu Okamura, Tatsuya Kikuchi, Ming-Rong Zhang
  • Total Pages: 1132
  • Publisher: Springer, Cham
  • ISBN: 9783030531768