Abstract
To develop a potential SPECT probe to evaluate the integrity of the serotoninergic system (5-HTT) whose dysfunction is linked to several disease conditions such as Parkinson's disease, Alzheimer's disease and depression, we report the synthesis, radiolabeling and in vivo baboon imaging of 2beta-carbomethoxy-3beta-(3'-[(123)I]iodophenyl) tropane (YP256, 6). The radiolabeling was performed by iododestannylation using sodium [(123)I]iodide and peracetic acid. Although the ligand displayed high selectivity for 5-HTT over dopamine transporter in vitro, SPECT imaging in baboons did not reveal selective 5-HTT accumulation in brain in vivo.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, Non-U.S. Gov't
-
Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
-
Animals
-
Brain / metabolism
-
Chromatography, High Pressure Liquid
-
Cocaine / analogs & derivatives*
-
Cocaine / chemical synthesis
-
Cocaine / metabolism
-
Female
-
Iodine Radioisotopes*
-
Isotope Labeling*
-
Papio
-
Radiopharmaceuticals / chemical synthesis*
-
Radiopharmaceuticals / metabolism
-
Serotonin Plasma Membrane Transport Proteins / metabolism*
-
Tomography, Emission-Computed, Single-Photon*
Substances
-
2-carbomethoxy-3-(3'-iodophenyl)tropane
-
Iodine Radioisotopes
-
Radiopharmaceuticals
-
Serotonin Plasma Membrane Transport Proteins
-
Cocaine