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556 results on '"Kumata, Katsushi"'

1. Imaging α-synuclein pathologies in animal models and patients with Parkinson’s and related diseases

Author

Endo, Hironobu, primary, Ono, Maiko, additional, Takado, Yuhei, additional, Matsuoka, Kiwamu, additional, Takahashi, Manami, additional, Tagai, Kenji, additional, Kataoka, Yuko, additional, Hirata, Kosei, additional, Takahata, Keisuke, additional, Seki, Chie, additional, Kokubo, Naomi, additional, Fujinaga, Masayuki, additional, Mori, Wakana, additional, Nagai, Yuji, additional, Mimura, Koki, additional, Kumata, Katsushi, additional, Kikuchi, Tatsuya, additional, Shimozawa, Aki, additional, Mishra, Sushil K., additional, Yamaguchi, Yoshiki, additional, Shimizu, Hiroshi, additional, Kakita, Akiyoshi, additional, Takuwa, Hiroyuki, additional, Shinotoh, Hitoshi, additional, Shimada, Hitoshi, additional, Kimura, Yasuyuki, additional, Ichise, Masanori, additional, Suhara, Tetsuya, additional, Minamimoto, Takafumi, additional, Sahara, Naruhiko, additional, Kawamura, Kazunori, additional, Zhang, Ming-Rong, additional, Hasegawa, Masato, additional, and Higuchi, Makoto, additional

Published
2024
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2. A novel monoacylglycerol lipase-targeted 18F-labeled probe for positron emission tomography imaging of brown adipose tissue in the energy network

Author

Cheng, Ran, Fujinaga, Masayuki, Yang, Jing, Rong, Jian, Haider, Ahmed, Ogasawara, Daisuke, Van, Richard S., Shao, Tuo, Chen, Zhen, Zhang, Xiaofei, Calderon Leon, Erick R., Zhang, Yiding, Mori, Wakana, Kumata, Katsushi, Yamasaki, Tomoteru, Xie, Lin, Sun, Shaofa, Wang, Lu, Ran, Chongzhao, Shao, Yihan, Cravatt, Benjamin, Josephson, Lee, Zhang, Ming-Rong, and Liang, Steven H.

Published
2022
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5. Synthesis and preliminary evaluation of novel 11C-labeled GluN2B-selective NMDA receptor negative allosteric modulators

Author

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, and Liang, Steven H

Published
2021
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11. Development of Novel 11C-Labeled Selective Orexin-2 Receptor Radioligands for Positron Emission Tomography Imaging

Author

Rong, Jian, primary, Yamasaki, Tomoteru, additional, Li, Yinlong, additional, Kumata, Katsushi, additional, Zhao, Chunyu, additional, Haider, Ahmed, additional, Chen, Jiahui, additional, Xiao, Zhiwei, additional, Fujinaga, Masayuki, additional, Hu, Kuan, additional, Mori, Wakana, additional, Zhang, Yiding, additional, Xie, Lin, additional, Zhou, Xin, additional, Collier, Thomas L., additional, Zhang, Ming-Rong, additional, and Liang, Steven, additional

Published
2023
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12. Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys

Author

Nagai, Yuji, Miyakawa, Naohisa, Takuwa, Hiroyuki, Hori, Yukiko, Oyama, Kei, Ji, Bin, Takahashi, Manami, Huang, Xi-Ping, Slocum, Samuel T., DiBerto, Jeffrey F., Xiong, Yan, Urushihata, Takuya, Hirabayashi, Toshiyuki, Fujimoto, Atsushi, Mimura, Koki, English, Justin G., Liu, Jing, Inoue, Ken-ichi, Kumata, Katsushi, Seki, Chie, Ono, Maiko, Shimojo, Masafumi, Zhang, Ming-Rong, Tomita, Yutaka, Nakahara, Jin, Suhara, Tetsuya, Takada, Masahiko, Higuchi, Makoto, Jin, Jian, Roth, Bryan L., and Minamimoto, Takafumi

Published
2020
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14. Reduced serotonergic transmission alters sensitivity to cost and reward via 5-HT1A and 5-HT1B receptors in monkeys.

Author

Hori, Yukiko, Mimura, Koki, Nagai, Yuji, Hori, Yuki, Kumata, Katsushi, Zhang, Ming-Rong, Suhara, Tetsuya, Higuchi, Makoto, and Minamimoto, Takafumi

Subjects
REWARD (Psychology), SEROTONIN, MACAQUES, ACTION theory (Psychology), POSITRON emission tomography, MONKEYS, SEROTONIN receptors
Abstract

Serotonin (5-HT) deficiency is a core biological pathology underlying depression and other psychiatric disorders whose key symptoms include decreased motivation. However, the exact role of 5-HT in motivation remains controversial and elusive. Here, we pharmacologically manipulated the 5-HT system in macaque monkeys and quantified the effects on motivation for goal-directed actions in terms of incentives and costs. Reversible inhibition of 5-HT synthesis increased errors and reaction times on goal-directed tasks, indicating reduced motivation. Analysis found incentive-dependent and cost-dependent components of this reduction. To identify the receptor subtypes that mediate cost and incentive, we systemically administered antagonists specific to 4 major 5-HT receptor subtypes: 5-HT1A, 5-HT1B, 5-HT2A, and 5-HT4. Positron emission tomography (PET) visualized the unique distribution of each subtype in limbic brain regions and determined the systemic dosage for antagonists that would achieve approximately 30% occupancy. Only blockade of 5-HT1A decreased motivation through changes in both expected cost and incentive; sensitivity to future workload and time delay to reward increased (cost) and reward value decreased (incentive). Blocking the 5-HT1B receptor also reduced motivation through decreased incentive, although it did not affect expected cost. These results suggest that 5-HT deficiency disrupts 2 processes, the subjective valuation of costs and rewards, via 5-HT1A and 5-HT1B receptors, thus leading to reduced motivation. Serotonin deficiency is a core biological pathology underlying depression and other psychiatric disorders whose key symptoms include decreased motivation. A model-based behavioral analysis with quantitatively controlled pharmacological manipulation in monkeys reveals differential contributions of the two serotonin receptor subtypes to reduced motivation in terms of cost-benefit trade-offs. [ABSTRACT FROM AUTHOR]

Published
2024
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28. Efficient radiosynthesis and non-clinical safety tests of the TSPO radioprobe [18F]FEDAC: Prerequisites for clinical application

Author

Kawamura, Kazunori, Kumata, Katsushi, Takei, Makoto, Furutsuka, Kenji, Hashimoto, Hiroki, Ito, Takehito, Shiomi, Satoshi, Fujishiro, Tomoya, Watanabe, Ryuji, Igarashi, Nobuyuki, Muto, Masatoshi, Yamasaki, Tomoteru, Yui, Joji, Xie, Lin, Hatori, Akiko, Zhang, Yiding, Nemoto, Kazuyoshi, Fujibayashi, Yasuhisa, and Zhang, Ming-Rong

Published
2016
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30. sj-pdf-1-jcb-10.1177_0271678X231152025 - Supplemental material for Small-animal PET study for noninvasive quantification of transmembrane AMPA receptor regulatory protein γ-8 (TARP γ-8) in the brain

Author

Yamasaki, Tomoteru, Ishii, Hideki, Hiraishi, Atsuto, Kumata, Katsushi, Wakizaka, Hidekatsu, Zhang, Yiding, Kurihara, Yusuke, Ogawa, Masanao, Nengaki, Nobuki, Chen, Jiahui, Li, Yinlong, Liang, Steven, and Zhang, Ming-Rong

Subjects
110320 Radiology and Organ Imaging, FOS: Clinical medicine, FOS: Biological sciences, Medicine, Cell Biology, 110305 Emergency Medicine, 110306 Endocrinology, Biochemistry, 69999 Biological Sciences not elsewhere classified, 110904 Neurology and Neuromuscular Diseases, Neuroscience
Abstract

Supplemental material, sj-pdf-1-jcb-10.1177_0271678X231152025 for Small-animal PET study for noninvasive quantification of transmembrane AMPA receptor regulatory protein γ-8 (TARP γ-8) in the brain by Tomoteru Yamasaki, Hideki Ishii, Atsuto Hiraishi, Katsushi Kumata, Hidekatsu Wakizaka, Yiding Zhang, Yusuke Kurihara, Masanao Ogawa, Nobuki Nengaki, Jiahui Chen, Yinlong Li, Steven Liang, Ming-Rong Zhang in Journal of Cerebral Blood Flow & Metabolism

Published
2023
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32. The Glutaminase-1 Inhibitor [ 11 C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice.

Author

Zhang, Yiding, Kumata, Katsushi, Xie, Lin, Kurihara, Yusuke, Ogawa, Masanao, Kokufuta, Tomomi, Nengaki, Nobuki, and Zhang, Ming-Rong

Subjects
*POSITRON emission tomography, *BENZYL chloride, *MAGNESIUM chloride, *MICE, *SMALL intestine, *THIADIAZOLES
Abstract

Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [11C-carbonyl]BPTES ([11C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [11C]BPTES was synthesized by the reaction of an amine precursor () with [11C-carbonyl]phenylacetyl acid anhydride ([11C]2), which was prepared from [11C]CO2 and benzyl magnesium chloride, followed by in situ treatment with isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [11C]BPTES was 9.5% (based on [11C]CO2) during a synthesis time of 40 min. A PET study with [11C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice. [ABSTRACT FROM AUTHOR]

Published
2023
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39. 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)

Author

Yamasaki, Tomoteru, Zhang, Xiaofei, Kumata, Katsushi, Zhang, Yiding, Deng, Xiaoyun, Fujinaga, Masayuki, Chen, Zhen, Mori, Wakana, Kuan, Hu, Wakizaka, Hidekatsu, Hatori, Akiko, Xie, Lin, Ogawa, Masanao, Nengaki, Nobuki, Van, Richard, Shao, Yihan, J. Sheffler, Douglas, D. P. Cosford, Nicholas, Liang, Huan, Ming-Rong, Zhang, Tomoteru, Yamasaki, Katsushi, Kumata, Masayuki, Fujinaga, Wakana, Mori, Hidekatsu, Wakizaka, Akiko, Hatori, Lin, Xie, Masanao, Ogawa, Nobuki, Nengaki, and Zhang, Ming-Rong

Abstract

Metabotropic glutamate receptor 2 (mGlu2) is a known target for treating several central nervous system (CNS) disorders. To develop a viable positron emission tomography (PET) ligand for mGlu2, we identified new candidates 5a–i that are potent negative allosteric modulators (NAMs) of mGlu2. Among these candidates, 4-(2-fluoro-4-methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide (5i, also named as [11C]MG2-1812) exhibited high potency, high subtype selectivity, and favorable lipophilicity. Compound 5i was labeled with positron-emitting carbon-11 (11C) to obtain [11C]5i in high radiochemical yield and high molar activity by O-[11C]methylation of the phenol precursor 12 with [11C]CH3I. In vitro autoradiography with [11C]5i showed heterogeneous radioactive accumulation in the brain tissue sections, ranked in the order: cortex > striatum > hippocampus > cerebellum ≫ thalamus > pons. PET study of [11C]5i indicated in vivo specific binding of mGlu2 in the rat brain. Based on the [11C]5i scaffold, further optimization for new candidates is underway to identify a more suitable ligand for imaging mGlu2.

Published
2020

40. Synthesis and Preliminary Studies of 11C-labeled Tetrahydro-1,7-Naphthyridine-2-Carboxamides for PET Imaging of Metabotropic Glutamate Receptor 2

Author

Zhang, Xiaofei, Zhang, Yiding, Chen, Zhen, Shao, Tuo, Van, Richard, Kumata, Katsushi, Deng, Xiaoyun, Fu, Hualong, Yamasaki, Tomoteru, Rong, Jian, Kuan, Hu, Hatori, Akiko, Xie, Lin, Yu, Qingzhen, Ye, Weijian, Xu, Hao, J. Sheffler, Douglas, D. P. Cosford, Nicholas, Shao, Yihan, Tang, Pingping, Lu, Wang, Ming-Rong, Zhang, Liang, Huan, Katsushi, Kumata, Tomoteru, Yamasaki, Akiko, Hatori, Lin, Xie, and Zhang, Ming-Rong

Abstract

Selective modulation of metabotropic glutamate receptor 2 (mGlu2) represents a novel therapeutic approach for treating brain disorders, including schizophrenia, depression, Parkinson’s disease (PD), Alzheimer’s disease (AD), drug abuse and addiction. Imaging mGlu2 using positron emission tomography (PET) would allow in vivo quantification under physiological and pathological conditions and facilitate drug discovery by enabling target engagement studies. However, to date, few successful efforts have been disclosed to visualize mGlu2 in vivo, indicating an unmet and urgent clinical need. Herein we report the synthesis and preclinical evaluation of a focused library of mGlu2 modulators amenable for radiolabeling. The promising candidate 4-(2,4-difluorophenyl)-7-((2-methoxypyridin -4-yl)methyl)-5,6,7,8-tetrahydro-1,7-naphthyridine-2-carboxamide (21b), exhibited high potency and excellent subtype selectivity, which was then evaluated by in vitro autoradiography and in vivo PET imaging studies after labeling with carbon-11. Ligand [11C]21b (also known as [11C]MG2-1904) demonstrated high brain uptake and excellent in vitro/in vivo specific binding towards mGlu2 with high metabolic stability in the brain. As proof-of-concept, our preliminary work demonstrated a successful example of visualizing mGlu2 in vivo derived from negative allosteric modulators (NAMs), which represents a promising chemotype for further development and optimization aimed for clinical translation.

Published
2020

43. Radiosynthesis and Evaluation of Cyclohexyl (5-(2-[11C-Carbonyl]acetamidobenzo[d]thiazol-6-yl)-2-Methylpyridin-3-yl)Carbamate ([11C]PK68) As a New Radioligand For Imaging Receptor-Interacting Protein 1 Kinase

Author

Yamasaki, Tomoteru, primary, Kumata, Katsushi, additional, Hiraishi, Atsuto, additional, Zhang, Yiding, additional, Wakizaka, Hidekatsu, additional, Kurihara, Yusuke, additional, Nengaki, Nobuki, additional, and Zhang, Ming-Rong, additional

Published
2022
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44. 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

Author

Mori, Wakana, Yamasaki, Tomoteru, Hattori, Yasushi, Zhang, Yiding, Kumata, Katsushi, Fujinaga, Masayuki, Hanyu, Masayuki, Nengaki, Nobuki, Zhang, Hong, and Ming-Rong, Zhang

Abstract

Mutations that increase leucine-rich repeat kinase 2 (LRRK2) activity in the brain are associated with Parkinson's disease. Here, we synthesized a novel compound 4-(6-fluoro-4-(5-isopropoxy-1H-indazol-3-yl)pyridin-2-yl)morpholine (FIPM) and labeled it with fluorine-18 (18F), to develop a positron emission tomography (PET) tracer for in vivo visualization of LRRK2 in the brain. FIPM showed high in vitro binding affinity for LRRK2 (IC50 = 8.0 nM). [18F]FIPM was prepared in 5% radiochemical yield (n = 5), by inserting 18F into a pyridine ring, followed by removal of the protecting group. After HPLC separation and formulation, [18F]FIPM was acquired with >97% radiochemical purity and 103–300 GBq μmol−1 of molar activity at the end of radiosynthesis. Biodistribution and small-animal PET studies in mice indicated a low in vivo specific binding of [18F]FIPM. While [18F]FIPM presented limited potential as an in vivo PET tracer for LRRK2, we suggested that it can be used as a lead compound for developing new radiotracers with improved in vivo brain properties.

Published
2020

47. Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold

Author

Rong, Jian, primary, Mori, Wakana, additional, Xia, Xiaotian, additional, Schafroth, Michael A., additional, Zhao, Chunyu, additional, Van, Richard S., additional, Yamasaki, Tomoteru, additional, Chen, Jiahui, additional, Xiao, Zhiwei, additional, Haider, Ahmed, additional, Ogasawara, Daisuke, additional, Hiraishi, Atsuto, additional, Shao, Tuo, additional, Zhang, Yiding, additional, Chen, Zhen, additional, Pang, Fuwen, additional, Hu, Kuan, additional, Xie, Lin, additional, Fujinaga, Masayuki, additional, Kumata, Katsushi, additional, Gou, Yuancheng, additional, Fang, Yang, additional, Gu, Shuyin, additional, Wei, Huiyi, additional, Bao, Liang, additional, Xu, Hao, additional, Collier, Thomas L., additional, Shao, Yihan, additional, Carson, Richard E., additional, Cravatt, Benjamin F., additional, Wang, Lu, additional, Zhang, Ming-Rong, additional, and Liang, Steven H., additional

Published
2021
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