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Novel radioiodinated sibutramine and fluoxetine as models for brain imaging

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Abstract

Brain imaging is a process which allows scientists and physicians to view and monitor the areas of the brain which allow diagnosis and following up different abnormalities in the brain. The aim of this study was to develop potential radiopharmaceuticals for the non-invasive brain imaging. Sibutramine and fluoxetine (two drugs that have the ability to cross blood–brain barrier) were successfully labeled with 125I via direct electrophilic substitution reaction at ambient temperature. The reaction parameters studied were substrate concentration, oxidizing agent concentration, pH of the reaction mixture, reaction temperature, reaction time and in vitro stability of the iodocompounds. The iodocompounds gave maximum labeling yield of 92 ± 2.77 and 93 ± 2.1%, respectively, and maintained stability throughout working period (24 h). Biodistribution studies showed that maximum in vivo uptake of the iodocompounds in the brain was 5.7 ± 0.19 and 6.14 ± 0.26% injected activity/g tissue organ, respectively, at 15 and 5 min post-injection, whereas the clearance from the mice appeared to proceed via the hepatobiliary pathway. Brain uptake of 125I-sibutramine and 125I-fluoxetine is higher than that of 99mTc-ECD and 99mTc-HMPAO (currently used radiopharmaceuticals for brain imaging) and so radioiodinated sibutramine and fluoxetine could be used instead of 99mTc-ECD and 99mTc-HMPAO for brain SPECT.

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Authors and Affiliations

  1. Labeled Compound Department, Hot Laboratory Center, Atomic Energy Authority, P.O. 13759, Cairo, Egypt

    M. A. Motaleb, M. T. El-Kolaly & H. M. Rashed

  2. Pharmaceutics Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt

    A. Abd El-Bary

Authors
  1. M. A. Motaleb
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  2. M. T. El-Kolaly
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  3. H. M. Rashed
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  4. A. Abd El-Bary
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Correspondence to M. A. Motaleb.

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Motaleb, M.A., El-Kolaly, M.T., Rashed, H.M. et al. Novel radioiodinated sibutramine and fluoxetine as models for brain imaging. J Radioanal Nucl Chem 289, 915–921 (2011). https://doi.org/10.1007/s10967-011-1182-z

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  • DOI: https://doi.org/10.1007/s10967-011-1182-z

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