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Synthesis of [2-11C]-6,7-dichloro-2,3-dihydroxyquinoxaline and evaluation of its in in vivo distribution in rat with PET

✍ Scribed by Jan-Olov Thorell; Sharon Stone-Elander; Martin Ingvar; Lars Eriksson

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
403 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A method for labelling 6,7‐dichloro‐2,3‐dihydroxyquinoxaline (DCQX) in position 2 with carbon‐11 is presented. Diethyl [1‐^11^C]oxalate was synthesized in a two‐step, microwave‐assisted procedure from no‐carrier‐added [^11^C]cyanide and was reacted with 4,5‐dichloro‐1,2‐phenylenediamine in sulfuric acid at 150°C for 10 min. [2‐^11^C]DCQX, isolated by semi‐preparative HPLC, was > 99% radiochemically pure with a specific activity ranging between 19 ‐ 26 TBq/mmol. The total time of synthesis was 45–55 min and the isolated, decay‐corrected yields were on the order of 10%, based on the trapped [^11^C]cyanide. A PET study of its biodistribution after intravenous injection in a male rat revealed that the extraction of [2^−11^C]DCQX across the intact blood‐brain barrier was ⩽ 2%.

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