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J-GLOBAL ID：201902269360881881   整理番号：19A0176836

一連のピラゾロ[1,5-a]ピリミジン類から誘導されたCNS penetrant MGlu_7/8受容体PAM,VU60649の発見【JST・京大機械翻訳】

Discovery of VU6005649, a CNS Penetrant mGlu_7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines

著者 (35件)： Abe Masahito (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Abe Masahito (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Seto Mabel (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Seto Mabel (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Gogliotti Rocco G. (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Gogliotti Rocco G. (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Loch Matthew T. (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Loch Matthew T. (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Bollinger Katrina A. (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Chang Sichen (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Engelberg Eileen M. (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Engelberg Eileen M. (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Luscombe Vincent B. (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Luscombe Vincent B. (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Harp Joel M. (Department of Biochemistry, Vanderbilt University School of Medicine, Tennessee, United States) ,  Bubser Michael (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Bubser Michael (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Engers Darren W. (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Engers Darren W. (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Jones Carrie K. (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Jones Carrie K. (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Jones Carrie K. (Vanderbilt Kennedy Center, Vanderbilt University Medical Center, Tennessee, United States) ,  Rodriguez Alice L. (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Rodriguez Alice L. (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Blobaum Anna L. (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Blobaum Anna L. (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Conn P. Jeffrey (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Conn P. Jeffrey (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Conn P. Jeffrey (Vanderbilt Kennedy Center, Vanderbilt University Medical Center, Tennessee, United States) ,  Niswender Colleen M. (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Niswender Colleen M. (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Niswender Colleen M. (Vanderbilt Kennedy Center, Vanderbilt University Medical Center, Tennessee, United States) ,  Lindsley Craig W. (Department of Pharmacology, Vanderbilt University School of Medicine, Tennessee, United States) ,  Lindsley Craig W. (Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Tennessee, United States) ,  Lindsley Craig W. (Vanderbilt Kennedy Center, Vanderbilt University Medical Center, Tennessee, United States)
資料名： ACS Medicinal Chemistry Letters  (ACS Medicinal Chemistry Letters)
巻： 8  号： 10  ページ： 1110-1115  発行年： 2017年 
JST資料番号： W5043A  ISSN： 1948-5875  資料種別： 逐次刊行物 (A)
記事区分： 短報  発行国： アメリカ合衆国 (USA)  言語： 英語 (EN)

抄録/ポイント： ここでは,優れたCNS浸透(K_ps>1およびK_p,UUS>1)を有するピラゾロ-[1,5-a]-ピリミジン核に基づく一連のmGlu_7 PAM内の構造-活性相関を報告する。このシリーズにおける類似体はグループIII mGlu受容体選択性の範囲を示すことが証明されたが,VU605649は第一の二重mGlu_7/8PAMとして出現し,グループIII mGlu受容体PAMツールボックスにボイドを充填し,マウス文脈恐怖条件付けモデルにおけるin vivo有効性を示した。Copyright 2019 American Chemical Society All rights reserved. Translated from English into Japanese by JST.【JST・京大機械翻訳】

シソーラス用語： 構造活性相関 ,  有効性 ,  浸透 ,  *受容体 ,  類似物質 ,  マウス
準シソーラス用語： 恐怖条件付け ,  ツールキット , 【Automatic Indexing@JST】

著者キーワード (5件)： 陽性アロステリック調節因子(PAM) ,  代謝型グルタミン酸受容体7(MGlu_7) ,  認知 ,  VU60649 ,  Rett症候群

分類 (2件)： 細胞膜の受容体  (EF04030C) ,  中枢神経系作用薬一般  (GW03010A)

タイトルに関連する用語 (5件)： ピリミジン類 ,  誘導 ,  受容体 ,  PAM ,  発見