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

✍ Scribed by V. Papazian; T. Jackson; T. Pham; X. Liu; I. Greguric; C. Loc'h; C. Rowe; V. Villemagne; C. L. Masters; A. Katsifis

Publisher
John Wiley and Sons
Year
2005
Tongue
French
Weight
154 KB
Volume
48
Category
Article
ISSN
0022-2135

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✦ Synopsis

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. ^123^I‐clioquinol (^123^I‐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 ^123^I‐CQ was purified by reverse‐phase HPLC using a C‐18 small ‘Rocket®’ column. The radiochemical purity of ^123^I‐CQ as assessed by analytical HPLC was 99.1±0.6% (n = 9) with specific activity higher than 3 GBq/nmol for ^123^I‐CQ and 80 MBq/nmol for ^125^I‐CQ. The total preparation time was 40 min and starting from 3.7 GBq of iodine‐123, more than 2.5 GBq of formulated ^123^I‐CQ as radiopharmaceutical was available for clinical investigations. Using the same method of preparation, ^125^I‐CQ was produced in radiochemical and chemical purity higher than 97% with a specific activity of 80 MBq/nmol. Copyright © 2005 John Wiley & Sons, Ltd.

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