Radiocomplexation, Quality Control and Bioevaluation of [99mTc]tricarbonyl Rolipram for Brain Imaging in Mice

被引:1
|
作者
Sanad, M. H. [1 ]
Eyssa, H. M. [2 ]
Abd-Elhaliem, S. M. [1 ]
Farag, A. B. [3 ]
Bassem, Sabry A. [4 ]
机构
[1] Egyptian Atom Energy Author, Hot Labs Ctr, Labeled Cpds Dept, Cairo 13759, Egypt
[2] Natl Ctr Radiat Res & Technol, Radiat Chem Dept, Cairo, Egypt
[3] Egyptian Atom Energy Author, Cairo 13759, Egypt
[4] Ahram Canadian Univ, Fac Pharm, Pharmaceut Chem Dept, Giza, Egypt
关键词
Rolipram; Tc-99m]tricarbonyl core; brain imaging; molecular modeling; docking; PEPTIC-ULCER; IN-VITRO; TC-99M;
D O I
10.1007/s11094-024-03190-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In this work, the complex of [Tc-99m]tricarbonyl rolipram was labeled utilizing a [Tc-99m]tricarbonyl core. Many optimal parameters have been used such as substrate (100 mu g), pH of the reaction mixture (pH 9), reaction time (30 min), as well as temperature (100 degrees C), providing an optimal radiochemical purity of 97.0%. Biodistribution investigations of our radiotracer, [Tc-99m]tricarbonyl rolipram, were conducted on normal Swiss Albino mice. The results indicated maximum brain uptakes of 8.2 %ID/g tissue at 10 min post injection (p.i.), which cleared from the brain with time until it reached 1.90 +/- 0.17% at 1 h p.i. Therefore, [Tc-99m]tricarbonyl rolipram complex may be an excessively bio-selective receptor-tracer for brain ulcer imaging through the phosphodiesterase-4 inhibitor.
引用
收藏
页码:652 / 660
页数:9
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