Oxidative radioiodination of meclofenoxate as a preclinical brain imaging agent

Meclofenoxate is a drug used to cause a broad improvement in brain function and mental performance. Meclofenoxate was successfully labeled with I via direct electrophilic substitution reaction at room temperature. Percent radiochemical yield was evaluated by paper electrophoresis and HPLC. The react...

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Bibliographic Details
Published inRadiochimica acta Vol. 104; no. 7; pp. 491 - 497
Main Authors El-Motaleb Abd El-Rhman, Mohamed Abd, Ibrahim, Ismail Taha, Abd El-Halim, Sayed Mohamed, El-Tawoosy, Mahmoud El-Sayed
Format Journal Article
LanguageEnglish
Published De Gruyter 28.07.2016
Subjects
biodistribution study
brain imaging
meclofenoxate
Radioiodination
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Summary:Meclofenoxate is a drug used to cause a broad improvement in brain function and mental performance. Meclofenoxate was successfully labeled with I 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-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 I-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-meclofenoxate was found to be enough to image brain as it still 4.3% ID/g at 30 min post injection.
ISSN:0033-8230
2193-3405
DOI:10.1515/ract-2015-2557