Synthesis and in vivo evaluation of [11C]CGP62349, a new GABAB receptor antagonist

被引：7

作者：

Todde, S

Moresco, RM

Fröstl, W

Stampf, P

Matarrese, M

Carpinelli, A

Magni, F

Kienle, MG

Fazio, F

机构：

[1] Univ Milano Bicocca, Sci Inst H San Rafaele, CNR, INB, Milan, Italy

[2] Novartis Pharma AG, CH-4002 Basel, Switzerland

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2000年 / 27卷 / 06期

关键词：

radiopharmaceuticals; GABA(B) receptors; PET; C-11; monkeys;

D O I：

10.1016/S0969-8051(00)00124-4

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：

This paper describes the radiosynthesis of [C-11]CGP62349, a potential ligand to assess GABA, receptors in vivo. C-11 was introduced by O-methylation of the corresponding des-methyl precursor, namely CGP67780. The final product was obtained with a reliable method in good yield. The radioligand was tested in monkey, revealing negligible blood brain barrier penetration and brain uptake, thus prompting us to search for a new target structure with a better lipophilicity. NUCL MED BIOL 27;6:565-569, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.

引用

页码：565 / 569

页数：5

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