Synthesis of [125I]iodoclorgyline, a selective monoamine oxidase A inhibitor, and its biodistribution in mice.
A new radioiodinated monoamine oxidase A (MAO-A) specific inhibitor, [125I]iodoclorgyline, was synthesized from its tin precursor by iododestannylation reaction using sodium [125I]iodide and hydrogen peroxide with high yield and site specificity. The product possessed a high radiochemical purity as well as high specific activity. The method can be readily applicable for labeling with 123I, a very suitable radioisotope for in vivo imaging with single photon emission computer tomography (SPECT). Biodistribution studies of the [125I]iodoclorgyline in mice showed high initial uptake in the brain, and brain radioactivity reached a constant level at 60 min after intravenous injection. The results suggested that [125I]iodoclorgyline might have potential as a radiopharmaceutical for MAO-A studies in the brain with SPECT.
Ohmomo
Y
Y
Osaka University of Pharmaceutical Sciences, Japan.
Hirata
M
M
Murakami
K
K
Magata
Y
Y
Tanaka
C
C
Yokoyama
A
A
D000818:Animals; D003010:Clorgyline / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D007457:Iodine Radioisotopes; D007553:Isotope Labeling; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D008995:Monoamine Oxidase / Q000378:metabolism; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution
D007457:Iodine Radioisotopes; D008996:Monoamine Oxidase Inhibitors; C074503:6-iodoclorgyline; D008995:Monoamine Oxidase; D003010:Clorgyline