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  1. 原著論文

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)

https://repo.qst.go.jp/records/80793
https://repo.qst.go.jp/records/80793
671795c0-8329-4557-bd2a-810e21a6e498
Item type 学術雑誌論文 / Journal Article(1)
公開日 2020-10-09
タイトル
タイトル 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)
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 Yamasaki, Tomoteru

× Yamasaki, Tomoteru

WEKO 1027178

Yamasaki, Tomoteru

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Zhang, Xiaofei

× Zhang, Xiaofei

WEKO 1027179

Zhang, Xiaofei

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Kumata, Katsushi

× Kumata, Katsushi

WEKO 1027180

Kumata, Katsushi

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Zhang, Yiding

× Zhang, Yiding

WEKO 1027181

Zhang, Yiding

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Deng, Xiaoyun

× Deng, Xiaoyun

WEKO 1027182

Deng, Xiaoyun

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Fujinaga, Masayuki

× Fujinaga, Masayuki

WEKO 1027183

Fujinaga, Masayuki

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Chen, Zhen

× Chen, Zhen

WEKO 1027184

Chen, Zhen

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Mori, Wakana

× Mori, Wakana

WEKO 1027185

Mori, Wakana

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Kuan, Hu

× Kuan, Hu

WEKO 1027186

Kuan, Hu

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Wakizaka, Hidekatsu

× Wakizaka, Hidekatsu

WEKO 1027187

Wakizaka, Hidekatsu

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Hatori, Akiko

× Hatori, Akiko

WEKO 1027188

Hatori, Akiko

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Xie, Lin

× Xie, Lin

WEKO 1027189

Xie, Lin

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Ogawa, Masanao

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WEKO 1027190

Ogawa, Masanao

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Nengaki, Nobuki

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WEKO 1027191

Nengaki, Nobuki

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Van, Richard

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WEKO 1027192

Van, Richard

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Shao, Yihan

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WEKO 1027193

Shao, Yihan

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J. Sheffler, Douglas

× J. Sheffler, Douglas

WEKO 1027194

J. Sheffler, Douglas

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D. P. Cosford, Nicholas

× D. P. Cosford, Nicholas

WEKO 1027195

D. P. Cosford, Nicholas

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Liang, Huan

× Liang, Huan

WEKO 1027196

Liang, Huan

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Ming-Rong, Zhang

× Ming-Rong, Zhang

WEKO 1027197

Ming-Rong, Zhang

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Tomoteru, Yamasaki

× Tomoteru, Yamasaki

WEKO 1027198

en Tomoteru, Yamasaki

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Katsushi, Kumata

× Katsushi, Kumata

WEKO 1027199

en Katsushi, Kumata

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Zhang, Yiding

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WEKO 1027200

en Zhang, Yiding

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Masayuki, Fujinaga

× Masayuki, Fujinaga

WEKO 1027201

en Masayuki, Fujinaga

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Wakana, Mori

× Wakana, Mori

WEKO 1027202

en Wakana, Mori

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Kuan, Hu

× Kuan, Hu

WEKO 1027203

en Kuan, Hu

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Hidekatsu, Wakizaka

× Hidekatsu, Wakizaka

WEKO 1027204

en Hidekatsu, Wakizaka

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Akiko, Hatori

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WEKO 1027205

en Akiko, Hatori

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Lin, Xie

× Lin, Xie

WEKO 1027206

en Lin, Xie

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Masanao, Ogawa

× Masanao, Ogawa

WEKO 1027207

en Masanao, Ogawa

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Nobuki, Nengaki

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WEKO 1027208

en Nobuki, Nengaki

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Liang, Huan

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WEKO 1027209

en Liang, Huan

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Zhang, Ming-Rong

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WEKO 1027210

en Zhang, Ming-Rong

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抄録
内容記述タイプ Abstract
内容記述 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.
書誌情報 Journal of Medicinal Chemistry

巻 2020, 号 63, p. 11469-11483, 発行日 2020-09
出版者
出版者 ACS Publications
ISSN
収録物識別子タイプ ISSN
収録物識別子 0022-2623
DOI
識別子タイプ DOI
関連識別子 10.1021/acs.jmedchem.9b01991
関連サイト
識別子タイプ URI
関連識別子 https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b01991
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