Radiosynthesis of novel carbon-11-labeled triaryl ligands for cannabinoid-type 2 receptor

被引：13

作者：

Fujinaga, Masayuki ^{[1
]}

Kumata, Katsushi ^{[1
]}

Yanamoto, Kazuhiko ^{[1
]}

Kawamura, Kazunori ^{[1
]}

Yamasaki, Tomoteru ^{[1
]}

Yui, Joji ^{[1
]}

Hatori, Akiko ^{[1
]}

Ogawa, Masanao ^{[1
,2
]}

Yoshida, Yuichiro ^{[1
,2
]}

Nengaki, Nobuki ^{[1
,2
]}

Maeda, Jun ^{[1
]}

Zhang, Ming-Rong ^{[1
]}

机构：

[1] Natl Inst Radiol Sci, Mol Imaging Ctr, Inage Ku, Chiba 2638555, Japan

[2] SHI Accelerator Serv Co Ltd, Shinagawa Ku, Tokyo 1418686, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 05期

关键词：

Cannabinoid subtype-2; PET; Triaryl ligands; Brain uptake; Radiosynthesis; CB2; RECEPTOR; BRAIN; RADIOLIGAND; MODULATION; EXPRESSION; BINDING; CELLS;

D O I：

10.1016/j.bmcl.2010.01.074

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two novel triaryl ligands 2 and 5 with potent in vitro binding affinities for the cannabinoid subtype-2 (CB2) receptor were labeled with a positron-emitting radioactive nuclide C-11. Radioligands [ 11C] 2, [C-11]5, and their analogs [C-11]3 and [C-11]4 were synthesized by O-[C-11]methylation of their corresponding phenol precursors with [C-11]CH3I. [C-11]2-5 had relatively high uptakes (>1.2% injected dose/g tissue) in mouse brains. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：1565 / 1568

页数：4

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