THE PRESENT study focused on synthesis of radioiodinated aniracetam for a potential brain imaging. Aniracetam (AN) has been labeled using [125I] with chloramine-T (Ch-T) as an oxidizing agent. The key effective factors such as amount of oxidizing agent, amount of substrate, pH, reaction temperature and reaction time, have been systematically studied to get high radiochemical yield of the radioiodinated aniracetam. The obtained results show a high radiochemical yield of iodoaniracetam that reached 98%. The labeled compound was separated and purified using thin layer chromatography (TLC), paper electrophoreses and high performance liquid chromatography (HPLC). Docking and modeling with AMPA receptors, gamma camera and drug inhibition were studied. In vivo biodistribution of radioiodinated aniracetam was evaluated in Swiss albino mice. The biodistribution results show a brain uptake that reached 9.50 ± 0.17 %ID/g at 15 min post injection (p.i.). Based on these results, it can be stated that radioiodinated aniracetam could be efficiently used as a potential radiotracer drug for brain imaging.