Oxidative radioiodination of meclofenoxate as a preclinical brain imaging agent

摘要

Meclofenoxate is a drug used to cause a broad improvement in brain function and mental performance. Meclofenoxate was successfully labeled with I-125 via direct electrophilic substitution reaction at room temperature. Percent radiochemical yield was evaluated by paper electrophoresis and HPLC. The reaction parameters affecting the preparation process were studied in details. I-125-meclofenoxate gave maximum percent radiochemical yield of about 95 +/- 1.0% with specific activity 1.9 mu Ci/mu g meclofenoxate and its stability was up to 4 h. Biodistribution studies showed that maximum uptake of I-125-meclofenoxate in the brain of mice was 4.27 +/- 0.3% injected dose ( ID)/g tissue organ at 15 min post-injection. This uptake of I-125-meclofenoxate was found to be enough to image brain as it still 4.3% ID/g at 30 min post injection.