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Anxiolytic activity has been associated with GABA A  α2 and α3 subunits. Several target compounds were identified and required in C‐14 labeled form to enable a better understanding of their drug metabolism and pharmacokinetic properties.  AZD7325  is a selective GABA A  α2 and α3 receptor modulator intended for the treatment of anxiety through oral administration. A great number of  AZD7325  metabolites were observed across species  in vivo , whose identification was aided by [ 14 C] AZD7325 . An interesting metabolic cyclization and aromatization pathway leading to the tricyclic core of  M9  and the oxidative pathways to  M10  and  M42  are presented.

journal of labelled compounds and radiopharmaceuticals

Synthesis of C‐14 labeled GABA A  α2/α3 selective partial agonists and the investigation of late‐occurring and long‐circulating metabolites of GABA A  receptor modulator AZD7325