Radiolabeled Nefiracetam for Brain Imaging: Chromatographic Separation, Bio-Evaluation and Preclinical Assessment Studies

In this work, the [^99mTc]tricarbonyl Nefiracetam complex was labeled using the [^99mTc]tricarbonyl core. Optimum conditions were implemented to achieve a radiochemical purity of 98.0% as—a substrate of 200 mg, a pH of 8, a reaction time of 30 min, and a temperature of 100°C. Biodistribution investigations of the [^99mTc]tricarbonyl Nefiracetam tracer were performed on Swiss Albino mice and revealed peak brain uptake of 9.5% ID/gram in group B, Alzheimer’s group at 30 min post-injection (p.i.), cleared to 1.30 ± 0.19% at 2 h post-injection. This suggests that the [^99mTc]tricarbonyl Nefiracetam complex may act as a highly bio-selective tracer for brain ulcer imaging via nefiracetam induced-N-methyl-D-aspartic acid (NMDA) receptor potentiation.