✦ LIBER ✦

Session 3: Radiopharmaceutical Chemistry - Halogens I

Publisher: John Wiley and Sons
Year: 2003
Tongue: French
Weight: 811 KB
Volume: 46
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.752

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✦ Synopsis

Positron Emission Tomography (PET) is a high-resolution, sensitive and non-invasive imaging technique that can be used in humans. It is the most advanced technology current ly available for studying in vivo molecular interactions and also represents the method of choice to assess the distribution and pharmacokinetics of proteins in vivo. The most widely used positronemitting radiohalogen is fluorine-18 (half-life : 109.8 minutes). Among the positron emitters, it is likely to be the radionuclide of choice for its physical and nuclear characteristics. However, apart from a few exceptions, its use precludes the "direct labelling" of macromolecules such as proteins and requires the design and development of dedicated fluorine-18 labelled prosthetic groups (1,2). Carboxylic acids and their succinimidyl derivatives are the most common reagents developped and dedicated to the labelling of amine functions (Lys -( e )NH2 essentially) via acylation reactions. In the present work, we have designed and synthesized a [

18 F]fluoropyridinyne-based maleimide reagent, [ 18 F]-1, for specific radioactive alkylation of thiol functions (Cys-SH).

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