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  1. 原著論文

A human PET study of [¹¹C]HMS011, a potential radioligand for AMPA receptors

https://repo.qst.go.jp/records/48777
https://repo.qst.go.jp/records/48777
68e1449f-6278-4b62-963a-b3ecaee9e412
Item type 学術雑誌論文 / Journal Article(1)
公開日 2018-04-23
タイトル
タイトル A human PET study of [¹¹C]HMS011, a potential radioligand for AMPA receptors
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 Takahata, Keisuke

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WEKO 491084

Takahata, Keisuke

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Kimura, Yasuyuki

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WEKO 491085

Kimura, Yasuyuki

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Seki, Chie

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WEKO 491086

Seki, Chie

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Tokunaga, Masaki

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WEKO 491087

Tokunaga, Masaki

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Ichise, Masanori

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WEKO 491088

Ichise, Masanori

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Kawamura, Kazunori

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WEKO 491089

Kawamura, Kazunori

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Ono, Maiko

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WEKO 491090

Ono, Maiko

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Kitamura, Soichiro

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WEKO 491091

Kitamura, Soichiro

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Kubota, Manabu

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WEKO 491092

Kubota, Manabu

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Moriguchi, Sho

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WEKO 491093

Moriguchi, Sho

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Ishii, Tatsuya

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WEKO 491094

Ishii, Tatsuya

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Takado, Yuhei

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WEKO 491095

Takado, Yuhei

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Niwa, Fumitoshi

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WEKO 491096

Niwa, Fumitoshi

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Endo, Hironobu

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WEKO 491097

Endo, Hironobu

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Nagashima, Tomohisa

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WEKO 491098

Nagashima, Tomohisa

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Ikoma, Yoko

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WEKO 491099

Ikoma, Yoko

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Zhang, Ming-Rong

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WEKO 491100

Zhang, Ming-Rong

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Suhara, Tetsuya

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WEKO 491101

Suhara, Tetsuya

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Higuchi, Makoto

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WEKO 491102

Higuchi, Makoto

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高畑 圭輔

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WEKO 491103

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木村 泰之

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関 千江

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徳永 正希

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WEKO 491106

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市瀬 正則

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河村 和紀

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小野 麻衣子

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北村 聡一郎

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久保田 学

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森口 翔

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石井 辰弥

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高堂 裕平

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丹羽 文俊

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遠藤 浩信

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永嶌 朋久

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生駒 洋子

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張 明栄

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須原 哲也

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樋口 真人

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抄録
内容記述タイプ Abstract
内容記述 Background: α-Amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor is a primary mediator of fast
glutamatergic excitatory signaling in the brain and has been implicated in diverse neuropsychiatric diseases. We
recently developed a novel positron emission tomography (PET) ligand, 2-(1-(3-([11C]methylamino)phenyl)-2-oxo-5-
(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl) benzonitrile ([11C]HMS011). This compound is a radiolabelled derivative of
perampanel, an antiepileptic drug acting on AMPA receptors, and was demonstrated to have promising in vivo
properties in the rat and monkey brains. In the current study, we performed a human PET study using [11C]HMS011
to evaluate its safety and kinetics.
Four healthy male subjects underwent a 120-min PET scan after injection of [11C]HMS011. Arterial blood sampling
and metabolite analysis were performed to obtain parent input functions for three of the subjects using highperformance
liquid chromatography. Regional distribution volumes (VTs) were calculated based on kinetic models
with and without considering radiometabolite in the brain. The binding was also quantified using a reference tissue
model with white matter as reference.
Results: Brain uptake of [11C]HMS011 was observed quickly after the injection, followed by a rapid clearance. Three
hydrophilic and one lipophilic radiometabolites appeared in the plasma, with notable individual variability. The kinetics
in the brain with apparent radioactivity retention suggested that the lipophilic radiometabolite could enter the brain. A
dual-input graphical model, an analytical model designed in consideration of a radiometabolite entering the brain, well
described the kinetics of [11C]HMS011. A reference tissue model showed small radioligand binding potential (BP*ND)
values in the cortical regions (BP*ND = 0–0.15). These data suggested specific binding component of [11C]HMS011 in
the brain.
Conclusions: Kinetic analyses support some specific binding of [11C]HMS011 in the human cortex. However, this ligand
may not be suitable for practical AMPA receptor PET imaging due to the small dynamic range and metabolite in the brain.
Keywords: PET, Perampanel, AMPA, [11C]HMS011, Interspecies differences
書誌情報 EJNMMI Research

巻 7, 号 63, 発行日 2017-08
出版者
出版者 Springer Berlin
ISSN
収録物識別子タイプ ISSN
収録物識別子 2191-219X
PubMed番号
識別子タイプ PMID
関連識別子 28815446
DOI
識別子タイプ DOI
関連識別子 10.1186/s13550-017-0313-0
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