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Large scale preparation strategy for labelling of [123I]-SCH 23982, a dopamine D1 receptor binding agent

✍ Scribed by H.-F. Beer; Sha Lin; I. Novak-Hofer; P. Bläuenstein; P.A. Schubiger

Publisher
Elsevier Science
Year
1992
Weight
475 KB
Volume
43
Category
Article
ISSN
0883-2889

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✦ Synopsis

The labelling of the D1 antagonist SCH 23982 with 123I was studied in detail by following the nucleophilic and electrophilic approaches and the reaction conditions were optimized. The product was purified by reversed phase HPLC with a phosphoric acid/EtOH mixture which simply has to be neutralized and diluted before injection. Its binding was tested in vitro with rat striatal membranes proving the high affinity to D1 and very low affinity to D2 receptors.

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Radiosynthesis of high effective specifi
Radiosynthesis of high effective specific-activity [123I]SCH 23982 for dopamine D-1 receptor-based SPECT imaging
✍ Stephen M. Moerlein; David Parkinson; Michael J. Welch 📂 Article 📅 1990 🏛 Elsevier Science ⚖ 478 KB

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