Journal article

The preparation of I-123/125-clioquinol for the study of A beta protein in Alzheimer's disease

V Papazian, T Jackson, T Pham, X Liu, I Greguric, C Loc'h, C Rowe, V Villemagne, CL Masters, A Katsifis

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | WILEY | Published : 2005

Abstract

Clioquinol or 5-chloro-7-iodo-8-hydroxyquinoline (CQ) is a lipophilic hydroxyquinoline currently under investigation for the treatment of Alzheimer's disease by targeted copper and zinc chelation. CQ was radiolabelled with no-carrier-added iodine-123/125 to give high specific activity analogs for SPECT imaging and biochemical studies. 123I-clioquinol ( 123I-CQ) was prepared by direct iodination of the activated hydroxyquinoline using a variety of oxidants. Highest yields (>85%) and purity were obtained when chloramine-T or iodogen at pH 4-5 was used. Large-scale radiolabelled 123I-CQ was purified by reverse-phase HPLC using a C-18 small 'Rocket®' column. The radiochemical purity of 123I-CQ a..

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