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

Physics

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