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.
Kiyono
Yasushi
Y
Radioisotopes Research Laboratory, Kyoto University Hospital, Faculty of Medicine, Kyoto University, Kyoto, Japan.
Kanegawa
Naoki
N
Kawashima
Hidekazu
H
Kitamura
Yoji
Y
Iida
Yasuhiko
Y
Saji
Hideo
H
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D001931:Brain Mapping; D005473:Fluoxetine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D007457:Iodine Radioisotopes / Q000493:pharmacokinetics; D007553:Isotope Labeling; D008024:Ligands; D008297:Male; D050484:Norepinephrine Plasma Membrane Transport Proteins; D009928:Organ Specificity; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D027981:Symporters / Q000378:metabolism*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods*
D007457:Iodine Radioisotopes; D008024:Ligands; C483738:N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine; D050484:Norepinephrine Plasma Membrane Transport Proteins; D019275:Radiopharmaceuticals; C493226:Slc6a2 protein, rat; D027981:Symporters; D005473:Fluoxetine