Radiosynthesis of high effective specific-activity [123I]SCH 23982 for dopamine D-1 receptor-based SPECT imaging.
The high yield, high-specific activity radiosynthesis of the dopaminergic D-1 receptor-binding ligand [123I]SCH 23982 is described. Using no-carrier-added iododeprotonation of the des-iodo precursor SKF 83692 and column-switching HPLC, [123I]SCH 23982 was isolated in 35-40% radiochemical yield with an effective specific activity of 2250-4000 Ci/mmol and an overall preparation time of 90 min. The procedure outlined here can be employed for the clinical production of [123I]SCH 23982 as a SPECT radiopharmaceutical, as well as [125I]SCH 23982 to be used for in vitro receptor-binding applications.
Moerlein
S M
SM
Edward Mallinckrodt Institute of Radiology, Washington University, St Louis, MO 63110.
Parkinson
D
D
Welch
M J
MJ
D000818:Animals; D001552:Benzazepines / Q000031:analogs & derivatives*; D001921:Brain / Q000000981:diagnostic imaging*; D018492:Dopamine Antagonists; D005260:Female; D066298:In Vitro Techniques; D007457:Iodine Radioisotopes; D007553:Isotope Labeling / Q000379:methods; D008254:Macaca nemestrina; D008297:Male; D011954:Receptors, Dopamine; D017447:Receptors, Dopamine D1; D015899:Tomography, Emission-Computed, Single-Photon
C049558:8-iodo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-ol; D001552:Benzazepines; D018492:Dopamine Antagonists; D007457:Iodine Radioisotopes; D011954:Receptors, Dopamine; D017447:Receptors, Dopamine D1