Total synthesis and evaluation of [18F] MHMZ

被引：29

作者：

Herth, Matthias M. ^{[1
]}

Debus, Fabian ^{[2
]}

Piel, Markus ^{[1
]}

Palner, Mikael ^{[3
]}

Knudsen, Gitte M. ^{[3
]}

Lueddens, Hartmut ^{[2
]}

Roesch, Frank ^{[1
]}

机构：

[1] Johannes Gutenberg Univ Mainz, Inst Nucl Chem, D-55128 Mainz, Germany

[2] Clin Res Grp, Dept Psychiat, D-55131 Mainz, Germany

[3] Rigshosp, Ctr Integrated Mol Brain Imaging, DK-2100 Copenhagen, Denmark

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 04期

关键词：

F-18] MHMZ; MDL; 100907; F-18] altanserin; 5-HT2A; antagonist; positron emission tomography; autoradiography;

D O I：

10.1016/j.bmcl.2007.12.054

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[F-18] fluoroethyltosylate ([F-18] FETos) was carried out in yields of similar to 90% synthesizing [F-18] MHMZ in a specific activity of similar to 50 MBq/ nmol with a starting activity of similar to 3 GBq. Overall radiochemical yield including [F-18] FETos synthon synthesis, [F-18] fluoroalkylation and preparing the injectable [ 18 F] MHMZ solution was 42% within a synthesis time of similar to 100 min. The novel compound showed excellent specific binding to the 5-HT2A receptor (K-i = 9.0 nM) in vitro and promising in vivo characteristics. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：1515 / 1519

页数：5

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