A rapid high yield synthesis of no-carrier-added (-)-[123I]iodocyanopindolol.
A convenient and efficient radiosynthesis of no-carrier-added [123I]labeled (-)iodocyanopindolol, (-)-[123I]ICYP, a high affinity beta adrenergic antagonist, is described. (-)-[123I]ICYP was synthesized by a modified chloramine-T radioiodination of (-)cyanopindolol followed by a novel reversed-phase HPLC purification that provided the radiopharmaceutical as a directly injectable solution. The total synthesis time was typically less than 45 min and provided (-)-[123I]ICYP in a 59% radiochemical yield (not corrected for decay). In view of its high affinity for the beta adrenergic receptor, (-)-[123I]ICYP is a potentially useful probe for SPECT evaluation of cardiac adrenergic receptor density.
Van Dort
M E
ME
Division of Nuclear Medicine, University of Michigan Medical School, Ann Arbor, 48109-0552.
Gildersleeve
D L
DL
Wieland
D M
DM
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis* / Q000302:isolation & purification; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D007457:Iodine Radioisotopes; D020120:Iodocyanopindolol; D007553:Isotope Labeling / Q000379:methods*; D010869:Pindolol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000302:isolation & purification
D000319:Adrenergic beta-Antagonists; D007457:Iodine Radioisotopes; D020120:Iodocyanopindolol; D010869:Pindolol