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 a
Radiosynthesis of high effective specific-activity [123I]SCH 23982 for dopamine D-1 receptor-based SPECT imaging
β Scribed by Stephen M. Moerlein; David Parkinson; Michael J. Welch
- Publisher
- Elsevier Science
- Year
- 1990
- Weight
- 478 KB
- Volume
- 41
- Category
- Article
- ISSN
- 0883-2889
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β¦ Synopsis
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.
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Recently there has been an increased urge towards y-labelled tracers for in vivo dopamine receptors studies in human brain with SPECT. As 99m Tc chelate compunds for that purpose remain wishfull thinking until now, only 123 I labelled molecules can actually fulfil the technical requirements of imagi