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syn-1-Amino-3-[ 18 F]fluorocyclobutane-1-carboxylic acid

Kam Leung

PMID: 21328730

Abstract:

A variety of 11C- and 18F-labeled amino acids have been studied for potential use in positron emission tomography (PET) oncology (1, 2). Most brain tumors show an increased uptake of amino acids as compared with normal brain tissue (3). These amino acids are composed of naturally occurring amino acids, such as l-[11C]leucine, l-[11C]methionine, and l-[11C]tyrosine, and non-natural amino acids, such as [11C]aminoisobutyric acid, [11C]1-aminocyclopentane-1-carboxylic acid, and [11C]1-aminocyclobutane-1-carboxylic acid. 123I-Labeled amino acids are also used in imaging in oncology (4-6). The natural amino acids are taken up by tumor cells through an energy-independent L-type amino acid transporter system and retained in tumor cells because of their higher than normal metabolic pathways, including incorporation into proteins (4). l-[11C]Methionine and [18F]fluorotyrosine have been widely used in the detection of tumors although neither are approved by the FDA. On the other hand, the non-natural amino acids are not metabolized but are taken up through both the L-type transporter and the energy-dependent A-type transporter (7). Therefore, they can accumulate intracellularly in high concentrations. anti-1-Amino-3-[18F]fluorocyclobutane-1-carboxylic acid (anti-[18F]FACBC) was shown to have a high tumor/brain ratio (8), and anti-[18F]FACBC has been studied in humans with PET tumor imaging (9). In this chapter, syn-1-Amino-3-[18F]fluorocyclobutane-1-carboxylic acid (syn-3-[18F]FACBC) has also been synthesized and studied as a potential PET brain tumor imaging agent (10).

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP41365757 1-Amino-3,3-diethoxypropane 1-Amino-3,3-diethoxypropane 41365-75-7 Price
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