Radioiodination and Biological Evaluation of Tizanidine as a Potential Brain Imaging Agent | ||||
| Arab Journal of Nuclear Sciences and Applications | ||||
| Article 13, Volume 51, Issue 2, April 2018, Page 107-115 PDF (494.24 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/ajnsa.2018.2178.1017 | ||||
 View on SCiNiTO | ||||
| Authors | ||||
Mai Mourad  1; Abeer Amin2; Hanan Elsabagh2; Gehad Genidy Mohamed3; Salah Abd El-Ghani Abo-El-Enein4
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| 1Centre of Radiation Oncology and Nuclear Medicine, Kasr Al-Ainy, Cairo, Egypt | ||||
| 2Labeled Compounds Department, Hot Labs Center, Egyptian Atomic Energy Authority, Cairo, Egypt | ||||
| 3Chemistry Department, Faculty of Science, Cairo University, Giza, Egypt | ||||
| 4Chemistry Department, Faculty of Science, Ain Shams University, Cairo, Egypt | ||||
| Abstract | ||||
| LABELING was carried out by direct iodination of tizanidine (100 µg) with radioiodine (125I) in a fast single step at room temperature, to produce 125I-tizanidine (125I-TZN). 50 µg chloramine-T (CAT) was used as an oxidizing agent to oxidize the iodide ion to the iodonium ion, at neutral pH = 7 within 15 min. A high radiochemical yield of 92.8 % ± 0.1 was obtained. 125I-TZN was stable for 2 h without detection of any by-products in the reaction mixture. The partition coefficient value of 125I-TZN was 2.21 ± 0.02, showing that it is very lipophilic and can easily cross the blood brain barrier. Biodistribution studies and in vivo imaging showed that the initial brain uptake correlated fairly well with the brain-binding affinity of the compound. The brain uptake of 125I-TZN was as high as 5.2 % and 8.0 % in biodistribution studies and in vivo imaging at 120 min post injection, respectively. Thus, 125I-TZN is promising in radioreceptor assays for brain imaging. | ||||
| Keywords | ||||
| Radioiodination; Tizanidine; Biodistribution; Brain Imaging; SPECT | ||||
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