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  1. 原著論文

Imaging of transmembrane AMPA receptor regulatory protein by positron emission tomography

https://repo.qst.go.jp/records/86471
https://repo.qst.go.jp/records/86471
cb6e170f-8195-4605-8e95-79f00ed70b1d
Item type 学術雑誌論文 / Journal Article(1)
公開日 2022-07-05
タイトル
タイトル Imaging of transmembrane AMPA receptor regulatory protein by positron emission tomography
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 Qingzhen, Yu,

× Qingzhen, Yu,

WEKO 1058940

Qingzhen, Yu,

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Katsushi, Kumata

× Katsushi, Kumata

WEKO 1058941

Katsushi, Kumata

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Jian, Rong,

× Jian, Rong,

WEKO 1058942

Jian, Rong,

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Zhen, Chen,

× Zhen, Chen,

WEKO 1058943

Zhen, Chen,

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Tomoteru, Yamasaki

× Tomoteru, Yamasaki

WEKO 1058944

Tomoteru, Yamasaki

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Jiahui, Chen,

× Jiahui, Chen,

WEKO 1058945

Jiahui, Chen,

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Zhiwei, Xiao,

× Zhiwei, Xiao,

WEKO 1058946

Zhiwei, Xiao,

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Hideki, Ishii

× Hideki, Ishii

WEKO 1058947

Hideki, Ishii

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Atsuto, Hiraishi

× Atsuto, Hiraishi

WEKO 1058948

Atsuto, Hiraishi

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Tuo, Shao,

× Tuo, Shao,

WEKO 1058949

Tuo, Shao,

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Zhang, Yiding

× Zhang, Yiding

WEKO 1058950

Zhang, Yiding

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Kuan, Hu

× Kuan, Hu

WEKO 1058951

Kuan, Hu

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Lin, Xie

× Lin, Xie

WEKO 1058952

Lin, Xie

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Masayuki, Fujinaga

× Masayuki, Fujinaga

WEKO 1058953

Masayuki, Fujinaga

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Chunyu, Zhao,

× Chunyu, Zhao,

WEKO 1058954

Chunyu, Zhao,

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Wakana, Mori

× Wakana, Mori

WEKO 1058955

Wakana, Mori

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Thomas, Collier,

× Thomas, Collier,

WEKO 1058956

Thomas, Collier,

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Ahmed, Haider,

× Ahmed, Haider,

WEKO 1058957

Ahmed, Haider,

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Susumu, Tomita,

× Susumu, Tomita,

WEKO 1058958

Susumu, Tomita,

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Zhang, Ming-Rong

× Zhang, Ming-Rong

WEKO 1058959

Zhang, Ming-Rong

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Steven, Liang,

× Steven, Liang,

WEKO 1058960

Steven, Liang,

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Katsushi, Kumata

× Katsushi, Kumata

WEKO 1058961

en Katsushi, Kumata

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Tomoteru, Yamasaki

× Tomoteru, Yamasaki

WEKO 1058962

en Tomoteru, Yamasaki

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Hideki, Ishii

× Hideki, Ishii

WEKO 1058963

en Hideki, Ishii

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Atsuto, Hiraishi

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WEKO 1058964

en Atsuto, Hiraishi

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Zhang, Yiding

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WEKO 1058965

en Zhang, Yiding

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Kuan, Hu

× Kuan, Hu

WEKO 1058966

en Kuan, Hu

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Lin, Xie

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WEKO 1058967

en Lin, Xie

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Masayuki, Fujinaga

× Masayuki, Fujinaga

WEKO 1058968

en Masayuki, Fujinaga

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Wakana, Mori

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WEKO 1058969

en Wakana, Mori

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Zhang, Ming-Rong

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WEKO 1058970

en Zhang, Ming-Rong

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抄録
内容記述タイプ Abstract
内容記述 ABSTRACT: The transmembrane α-amino-3-hydroxyl-5-methyl-4-isoxazolepropionic acid (AMPA) receptor regulatory protein γ-8 (TARP γ-8)
constitutes an auxiliary subunit of AMPA receptors, which mediates various
brain functions including learning and memory. TARP γ-8 has emerged as a
promising therapeutic target for central nervous system disorders. Despite
considerable efforts, previously reported TARP γ-8 PET radioligands, such as
[
11C]TARP-1903 and [11C]TARP-1811 series, were plagued by limited brain
uptake and/or high nonspecific binding in vivo. Herein, we developed two
novel 11C-labeled probes, [11C]8 and [11C]15 (also named as [11C]TARP2105), of which the latter exhibited a reasonable brain uptake as well as
specific binding toward TARP γ-8 both in vitro and in vivo, as confirmed by
blocking experiments with the commercially available TARP γ-8 inhibitor,
JNJ-55511118 in the TARP γ-8-rich hippocampus. Overall, [11C]15 exhibited
promising tracer characteristics and proved to be a lead positron-emission tomography ligand for the non-invasive quantification of
TARP γ-8 in the mammalian brain.
書誌情報 Journal of Medicinal Chemistry

巻 65, 号 13, p. 9144-9158, 発行日 2022-06
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 0022-2623
DOI
識別子タイプ DOI
関連識別子 10.1021/acs.jmedchem.2c00377
関連サイト
識別子タイプ DOI
関連識別子 https://doi.org/10.1021/acs.jmedchem.2c00377
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