Synthesis of N ‐acetyl‐L‐aspartyl‐L‐glutamic acid; [3H]NAAG

[3H]NAAG,N-acetyl-L-aspartyl-L-glutamic acid has been widely used as a substrate in glutamate carboxypeptidase II (GCPII) reactions, either to determine the inhibitory constants at 50% inhibition (IC50) of novel compounds or to measure GCPII activities in different tissues harvested from various disease models. The importance of [3H]NAAG, combined with its current commercial unavailability, prompted the development of a reliable eight-step synthetic procedure towards [3H2]NAAG starting from commercially available pyroglutamate. Pure [3H]NAAG of high molar activity (49.8 Ci/mmol) and desired stereochemistry was isolated in high radiochemical yield (67 mCi) and radiochemical purity (>99%). The identity was confirmed by mass spectrometry and co-injection with unlabeled reference.

Source: Journal of Labelled Compounds and Radiopharmaceuticals - July 19, 2022 Category: Biochemistry Authors: Michal Kriegelstein, Ale š Marek Tags: RESEARCH ARTICLE Source Type: research