Carbon-11 labeled radioligands for imaging brain cannabinoid receptors

被引:24
作者
Mathews, WB [1 ]
Scheffel, U
Rauseo, PA
Ravert, HT
Frank, RA
Ellames, GJ
Herbert, JM
Barth, F
Rinaldi-Carmona, M
Dannals, RF
机构
[1] Johns Hopkins Univ, Dept Radiol, Baltimore, MD 21287 USA
[2] Sanofi Synthelabo, Malvern, PA 19355 USA
[3] Sanofi Synthelabo, Alnwick NE66 2JH, Northd, England
[4] Sanofi Synthelabo, Montpellier 04, France
关键词
antagonist; cannabinoid; carbon-11; CB1; mice; PET;
D O I
10.1016/S0969-8051(02)00308-6
中图分类号
R8 [特种医学]; R445 [影像诊断学];
学科分类号
1002 ; 100207 ; 1009 ;
摘要
Two radioligands, [C-11] SR149080 and its morpholino analog [C-11] SR149568, were synthesized by reaction of the respective phenolic precursors with [C-11] methyl iodide. Both radioligands had appropriate regional brain distribution for cannabinoid receptor's in mice with peak target to non-target ratios of 2.2 for [C-11] SR149080 and 1.6 for [C-11] SR149568 at 90 and 30 minutes post-injection respectively. The uptake of both tracers was blocked with a 1 mg/kg dose of SR141716A. (C) 2002 Elsevier Science Inc. All rights reserved.
引用
收藏
页码:671 / 677
页数:7
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