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NPY Yl receptor (NPY Y1-R) is\nthe most widely studied NPY receptor, and is involved in many of these processes.\nBMS-193885 (1) was previously developed as a potent and selective NPY Y1-R\nantagonist, which has good systemic bioavailability and brain penetration. To evaluate\nthe characteristics of 1 in vivo, we developed 11C-labeled BMS-193885 ([11C]1) and its\ndesmethyl analog ([11C]2) for potential use as two new positron emission tomography\n(PET) tracers.\nResults: [11C]1 was synthesized from [11C]methyl iodide using 2. [11C]2 was\nsynthesized from [11C]phosgene using its aniline and amine derivatives. The mean\n± S.D. decay-corrected radiochemical yields of [11C]1 and [11C]2 from 11CO2 at the\nend of radionuclide production were 23 ± 3.2% (n = 6) and 24 ± 1.5% (n = 4),\nrespectively. In biodistribution on mice, radioactivity levels for both tracers were\nrelatively high in the kidney, small intestine, and liver at 60 min post-injection. The\nradioactivity levels in the kidney, lung, and spleen of mice at 30 min post-injection\nwith [11C]1 were significantly reduced by pretreatment with 1 (10 mg/kg), and levels of\n[11C]1 in the brain of mice were significantly increased by pretreatment with the\nP-glycoprotein and breast cancer resistance protein inhibitor elacridar (10 mg/kg).\nIn metabolite analysis using mouse plasma, [11C]1 and [11C]2 were rapidly\nmetabolized within 30 min post-injection, and [11C]1 was mainly metabolized\ninto unlabeled 2 and radiolabeled components.\nConclusion: [11C]1 and [11C]2 were successfully synthesized with sufficient amount\nof radioactivity and high quality for use in vivo. Our study of [11C]1 and its desmethyl\nanalog [11C]2 was useful in that it helped to elucidate the in vivo characteristics of 1.\nKeywords: Carbon-11, Positron emission tomography, Neuropeptide Y1 receptor,\nBMS-193885", "subitem_description_type": "Abstract"}]}, "item_8_publisher_8": {"attribute_name": "出版者", "attribute_value_mlt": [{"subitem_publisher": "Springer"}]}, "item_8_relation_14": {"attribute_name": "DOI", "attribute_value_mlt": [{"subitem_relation_type_id": {"subitem_relation_type_id_text": "10.1186/s41181-019-0056-5", "subitem_relation_type_select": "DOI"}}]}, "item_8_source_id_9": {"attribute_name": "ISSN", "attribute_value_mlt": [{"subitem_source_identifier": "2365-421X", "subitem_source_identifier_type": "ISSN"}]}, "item_access_right": {"attribute_name": "アクセス権", "attribute_value_mlt": [{"subitem_access_right": "metadata only access", "subitem_access_right_uri": "http://purl.org/coar/access_right/c_14cb"}]}, "item_creator": {"attribute_name": "著者", "attribute_type": 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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/734249f0821d6-6bec-44e3-933f-9dd0d16386ce
Item type | 学術雑誌論文 / Journal Article(1) | |||||
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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× Mori, Wakana× Fujinaga, Masayuki× Yamasaki, Tomoteru× Zhang, Yiding× Wakizaka, Hidekatsu× Hatori, Akiko× Xie, Lin× Kumata, Katsushi× Ohkubo, Takayuki× Kurihara, Yusuke× Ogawa, Masanao× Nengaki, Nobuki× Ming-Rong, Zhang× Kawamura, Kazunori× Mori, Wakana× Fujinaga, Masayuki× Yamasaki, Tomoteru× Zhang, Yiding× Wakizaka, Hidekatsu× Hatori, Akiko× Xie, Lin× Kumata, Katsushi× Ohkubo, Takayuki× Kurihara, Yusuke× Ogawa, Masanao× Nengaki, Nobuki× 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 |
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書誌情報 |
EJNMMI Radiopharmacy and Chemistry 巻 4, 号 4, 発行日 2019-02 |
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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 |