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Radiocomplexation and Biological Evaluation of [99mTc]Tricarbonyl Rabeprazole as a Radiotracer for Peptic Ulcer Localization

Abstract

The radiotracer [99mTc]tricarbonyl Rabeprazole was successfully prepared using the [99mTc]tricarbonyl precursor. The reaction conditions were optimized (200 µg/2 mL substrate concentration, pH 8, incubation temperature 100°C, 30 min) to achieve the maximum radiochemical purity of 98%. Thin layer chromatography (TLC) and high-performance liquid chromatography (HPLC) were used to assess the radiochemical purity and quality control parameters. A biodistribution study was also conducted to evaluate the biological biodistribution of [99mTc]tricarbonyl Rabeprazole in three different groups of mice models, with the normal group serving as the control and the second and third groups being microbial and chemically induced stomach ulcer disease models, respectively. The radiotracer [99mTc]tricarbonyl Rabeprazole complex was administered intravenously into mice via the tail vein and dissected at predefined time intervals. The biodistribution data demonstrated that the maximum absorption of [99mTc]tricarbonyl Rabeprazole complex in the stomach of normal mice and microbially and chemically induced ulcerated mice were 9.5, 35.3, and 23.7% ID/g tissue at 1 h post injection, respectively. The outcomes of the research show that [99mTc]tricarbonyl Rabeprazole can be used as a promising imaging agent to diagnose stomach ulcers.

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Sanad, M.H., Marzook, F.A., Mandal, S.K. et al. Radiocomplexation and Biological Evaluation of [99mTc]Tricarbonyl Rabeprazole as a Radiotracer for Peptic Ulcer Localization. Radiochemistry 64, 211–218 (2022). https://doi.org/10.1134/S1066362222020138

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Keywords:

  • Rabeprazole
  • [99mTc]tricarbonyl precursor
  • labeling
  • Helicobacter pylori