Evaluation of radioiodinated (R)-N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine as a ligand for brain norepinephrine transporter imaging.

(R)-N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine (MIPP) was evaluated as a radiopharmaceutical for investigating brain norepinephrine transporters (NET) by single photon emission computed tomography (SPECT). (R)-[(125)I]MIPP was synthesized with high radiochemical yield (60%) and high radiochemical purity (> 98%). In biodistribution experiments, (R)-[(125)I]MIPP indicated that the brain uptake of (R)-[(125)I]MIPP was rapid and retained, and that the regional cerebral distribution was consistent with the density of NET. Moreover, the administration of desipramine decreased the accumulation of (R)-[(125)I]MIPP in the brain. HPLC analysis of brain radioactivity showed that more than 90% was intact (R)-MIPP. These results suggested that (R)-[(123)I]MIPP is a potential radiopharmaceutical for imaging brain NET.