Radioiodination and biological evaluation of tizanidine as a potential brain imaging agent
Joint Authors
Muhammad, G. G.
Murad, M. A.
Abu al-Aynayn, S. A.
Abd al-Aziz, H.
Amin, A. M.
Source
Arab Journal of Nuclear Sciences and Applications
Issue
Vol. 51, Issue 2 (30 Apr. 2018), pp.107-115, 9 p.
Publisher
The Egyptian Society of Nuclear Science and Applications
Publication Date
2018-04-30
Country of Publication
Egypt
No. of Pages
9
Main Subjects
Topics
Abstract EN
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.
American Psychological Association (APA)
Murad, M. A.& Abd al-Aziz, H.& Amin, A. M.& Muhammad, G. G.& Abu al-Aynayn, S. A.. 2018. Radioiodination and biological evaluation of tizanidine as a potential brain imaging agent. Arab Journal of Nuclear Sciences and Applications،Vol. 51, no. 2, pp.107-115.
https://search.emarefa.net/detail/BIM-899642
Modern Language Association (MLA)
Abu al-Aynayn, S. A.…[et al.]. Radioiodination and biological evaluation of tizanidine as a potential brain imaging agent. Arab Journal of Nuclear Sciences and Applications Vol. 51, no. 2 (Apr. 2018), pp.107-115.
https://search.emarefa.net/detail/BIM-899642
American Medical Association (AMA)
Murad, M. A.& Abd al-Aziz, H.& Amin, A. M.& Muhammad, G. G.& Abu al-Aynayn, S. A.. Radioiodination and biological evaluation of tizanidine as a potential brain imaging agent. Arab Journal of Nuclear Sciences and Applications. 2018. Vol. 51, no. 2, pp.107-115.
https://search.emarefa.net/detail/BIM-899642
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references : p. 114-115
Record ID
BIM-899642