Oxidative radioiodination of meclofenoxate as a preclinical brain imaging agent

Abstract

Abstract Meclofenoxate is a drug used to cause a broad improvement in brain function and mental performance. Meclofenoxate was successfully labeled with 125I 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. 125I-meclofenoxate gave maximum percent radiochemical yield of about 95 ± 1.0% with specific activity 1.9 μCi/μg meclofenoxate and its stability was up to 4 h. Biodistribution studies showed that maximum uptake of 125I-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 125I-meclofenoxate was found to be enough to image brain as it still 4.3% ID/g at 30 min post injection.