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In Vivo Evaluation of Limiting Brain Penetration of Probes for alpha2C-Adrenoceptor Using Small-Animal Positron Emission Tomography
https://repo.qst.go.jp/records/45865
https://repo.qst.go.jp/records/45865f9d31336-22bc-4086-bfef-4fa85d8269c0
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2010-07-26 | |||||
| タイトル | ||||||
| タイトル | In Vivo Evaluation of Limiting Brain Penetration of Probes for alpha2C-Adrenoceptor Using Small-Animal 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 |
Kawamura, Kazunori
× Kawamura, Kazunori× Akiyama, Mugumi× Yui, Joji× Yamasaki, Tomoteru× Hatori, Akiko× Kumata, Katsushi× Wakizaka, Hidekatsu× Takei, Makoto× Nengaki, Nobuki× Yanamoto, Kazuhiko× Fukumura, Toshimitsu× Zhang, Ming-Rong× 河村 和紀× 秋山 めぐみ× 由井 譲二× 山崎 友照× 羽鳥 晶子× 熊田 勝志× 脇坂 秀克× 武井 誠× 念垣 信樹× 柳本 和彦× 福村 利光× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | To evaluate in vivo brain penetration of alpha2C-adrenoceptor (alpha2C-AR) antagonists as a therapeutic agent, we synthesized two new 11C-labeled selective alpha2C-AR antagonists 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methyl-2-aryl-7-methoxybenzofuran ([11C]MBF) and acridin-9-yl-[4-(4-methylpiperazin-1-yl)phenyl]amine ([11C]JP-1302) as alpha2C-AR-selective positron emission tomography (PET) probes. The radiochemical yield, specific activity, and radiochemical purity of these probes was appropriate for injection. To evaluate whether the brain penetration of these probes is related to the function of two major drug efflux transporters, P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), we performed PET studies using wild-type and P-gp/Bcrp knockout mice. In wild-type mice, the radioactivity level after injection with [11C]MBF initially increased and effluxed immediately from the brain, whereas that with [11C]JP-1302 was distributed throughout the brain. However, the regional distribution of radioactivity after injection with [11C]JP-1302 in the brain was different from that of alpha2C-ARs. In P-gp/Bcrp knockout mice, uptake of [11C]MBF was approximately 3.7-fold higher and that of [11C]JP-1302 was approximately 1.6-fold higher than those in wild-type mice. These results indicate that brain penetration of the two PET probes was affected by modulation of P-gp and Bcrp functions. | |||||
| 書誌情報 |
ACS Chemical Neuroscience (Online Only URL:http://pubs.acs.org/journal/acncdm) 巻 1, 号 7, p. 520-528, 発行日 2010-06 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 1948-7193 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1021/cn1000364 | |||||
