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  1. 原著論文

Radiosynthesis and in vivo evaluation of 11C-labeled BMS-193885 and its desmethyl analog as PET tracers for neuropeptide Y1 receptors

https://repo.qst.go.jp/records/73424
https://repo.qst.go.jp/records/73424
9f0821d6-6bec-44e3-933f-9dd0d16386ce
Item type 学術雑誌論文 / Journal Article(1)
公開日 2019-02-20
タイトル
タイトル Radiosynthesis and in vivo evaluation of 11C-labeled BMS-193885 and its desmethyl analog as PET tracers for neuropeptide Y1 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 Kawamura, Kazunori

× Kawamura, Kazunori

WEKO 747411

Kawamura, Kazunori

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Mori, Wakana

× Mori, Wakana

WEKO 747412

Mori, Wakana

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Fujinaga, Masayuki

× Fujinaga, Masayuki

WEKO 747413

Fujinaga, Masayuki

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Yamasaki, Tomoteru

× Yamasaki, Tomoteru

WEKO 747414

Yamasaki, Tomoteru

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Zhang, Yiding

× Zhang, Yiding

WEKO 747415

Zhang, Yiding

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Wakizaka, Hidekatsu

× Wakizaka, Hidekatsu

WEKO 747416

Wakizaka, Hidekatsu

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Hatori, Akiko

× Hatori, Akiko

WEKO 747417

Hatori, Akiko

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Xie, Lin

× Xie, Lin

WEKO 747418

Xie, Lin

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Kumata, Katsushi

× Kumata, Katsushi

WEKO 747419

Kumata, Katsushi

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Ohkubo, Takayuki

× Ohkubo, Takayuki

WEKO 747420

Ohkubo, Takayuki

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Kurihara, Yusuke

× Kurihara, Yusuke

WEKO 747421

Kurihara, Yusuke

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Ogawa, Masanao

× Ogawa, Masanao

WEKO 747422

Ogawa, Masanao

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Nengaki, Nobuki

× Nengaki, Nobuki

WEKO 747423

Nengaki, Nobuki

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Ming-Rong, Zhang

× Ming-Rong, Zhang

WEKO 747424

Ming-Rong, Zhang

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Kawamura, Kazunori

× Kawamura, Kazunori

WEKO 747425

en Kawamura, Kazunori

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Mori, Wakana

× Mori, Wakana

WEKO 747426

en Mori, Wakana

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Fujinaga, Masayuki

× Fujinaga, Masayuki

WEKO 747427

en Fujinaga, Masayuki

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Yamasaki, Tomoteru

× Yamasaki, Tomoteru

WEKO 747428

en Yamasaki, Tomoteru

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Zhang, Yiding

× Zhang, Yiding

WEKO 747429

en Zhang, Yiding

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Wakizaka, Hidekatsu

× Wakizaka, Hidekatsu

WEKO 747430

en Wakizaka, Hidekatsu

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Hatori, Akiko

× Hatori, Akiko

WEKO 747431

en Hatori, Akiko

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Xie, Lin

× Xie, Lin

WEKO 747432

en Xie, Lin

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Kumata, Katsushi

× Kumata, Katsushi

WEKO 747433

en Kumata, Katsushi

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Ohkubo, Takayuki

× Ohkubo, Takayuki

WEKO 747434

en Ohkubo, Takayuki

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Kurihara, Yusuke

× Kurihara, Yusuke

WEKO 747435

en Kurihara, Yusuke

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Ogawa, Masanao

× Ogawa, Masanao

WEKO 747436

en Ogawa, Masanao

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Nengaki, Nobuki

× Nengaki, Nobuki

WEKO 747437

en Nengaki, Nobuki

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Ming-Rong, Zhang

× Ming-Rong, Zhang

WEKO 747438

en Ming-Rong, Zhang

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抄録
内容記述タイプ Abstract
内容記述 Background: Neuropeptide Y (NPY) has been implicated in a wide variety of
physiological processes, including feeding, learning, memory, emotion, cardiovascular
homeostasis, hormone secretion, and circadian rhythms. NPY Yl receptor (NPY Y1-R) is
the most widely studied NPY receptor, and is involved in many of these processes.
BMS-193885 (1) was previously developed as a potent and selective NPY Y1-R
antagonist, which has good systemic bioavailability and brain penetration. To evaluate
the characteristics of 1 in vivo, we developed 11C-labeled BMS-193885 ([11C]1) and its
desmethyl analog ([11C]2) for potential use as two new positron emission tomography
(PET) tracers.
Results: [11C]1 was synthesized from [11C]methyl iodide using 2. [11C]2 was
synthesized from [11C]phosgene using its aniline and amine derivatives. The mean
± S.D. decay-corrected radiochemical yields of [11C]1 and [11C]2 from 11CO2 at the
end of radionuclide production were 23 ± 3.2% (n = 6) and 24 ± 1.5% (n = 4),
respectively. In biodistribution on mice, radioactivity levels for both tracers were
relatively high in the kidney, small intestine, and liver at 60 min post-injection. The
radioactivity levels in the kidney, lung, and spleen of mice at 30 min post-injection
with [11C]1 were significantly reduced by pretreatment with 1 (10 mg/kg), and levels of
[11C]1 in the brain of mice were significantly increased by pretreatment with the
P-glycoprotein and breast cancer resistance protein inhibitor elacridar (10 mg/kg).
In metabolite analysis using mouse plasma, [11C]1 and [11C]2 were rapidly
metabolized within 30 min post-injection, and [11C]1 was mainly metabolized
into unlabeled 2 and radiolabeled components.
Conclusion: [11C]1 and [11C]2 were successfully synthesized with sufficient amount
of radioactivity and high quality for use in vivo. Our study of [11C]1 and its desmethyl
analog [11C]2 was useful in that it helped to elucidate the in vivo characteristics of 1.
Keywords: Carbon-11, Positron emission tomography, Neuropeptide Y1 receptor,
BMS-193885
書誌情報 EJNMMI Radiopharmacy and Chemistry

巻 4, 号 4, 発行日 2019-02
出版者
出版者 Springer
ISSN
収録物識別子タイプ ISSN
収録物識別子 2365-421X
DOI
識別子タイプ DOI
関連識別子 10.1186/s41181-019-0056-5
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