Facile one-pot strategy for brain imaging using radiolabeled [99mTc]-tricarbonyl histamine complex in Mice.

Sanad, M.H.; Eyssa, H. M.; Challan, Safaa B.; Farag, A. B.; Abdou, Fatma Y.; Soliman, Aiten M.; Abd-Elhaliem, S. M.; El Bakary, Nermeen M.

doi:10.21608/ejchem.2024.283339.9602

	Facile one-pot strategy for brain imaging using radiolabeled [99mTc]-tricarbonyl histamine complex in Mice.
Egyptian Journal of Chemistry
Volume 68, Issue 3, March 2025, Pages 37-50 PDF (780.59 K)
Document Type: Original Article
DOI: 10.21608/ejchem.2024.283339.9602
Authors
M.H. Sanad¹; H. M. Eyssa²; Safaa B. Challan^* ¹; A. B. Farag³; Fatma Y. Abdou⁴; Aiten M. Soliman⁴; S. M. Abd-Elhaliem¹; Nermeen M. El Bakary⁵
¹Labeled Compound Department, Hot Laboratory Centre, Egyptian Atomic Energy Authority, P.O. Box 13755, Cairo, Egypt
²Radiation Chemistry Department, National Centre for Radiation Research and Technology, Egyptian Atomic Energy, Authority, P.O. Box 11787, Cairo, Egypt.
³Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ahram Canadian University, Giza, 12578 Egypt.
⁴Drug Radiation Research Department, National Centre for Radiation Research and Technology, Egyptian Atomic Energy, Authority, P.O. Box 11787, Cairo, Egypt.
⁵Radiation Biology Department, National Centre for Radiation Research and Technology, Egyptian Atomic Energy Authority, P.O. Box 11787, Cairo, Egypt.
Abstract
This investigation aims to label the histamine ligand, 2-(1H-imidazol-4-yl) ethanamine, using a [99mTc]-tricarbonyl core method for brain imaging. The optimization of all variables and factors influencing the radiochemical reaction is carried out to produce the labeled compound with a high radiochemical yield of 98.5%. The radiolabeled compound was stable for up to 6 hours, with a logarithm of the partition coefficient value at 1.49 ± 0.04. This value suggests the lipophilic characteristics of the [99mTc]-tricarbonyl histamine compound, indicating its potential to cross the blood-brain barrier effectively. The bioevaluation of the radiotracer [99mTc]-tricarbonyl-histamine complex exhibited a notable brain uptake of 8.5% ID/organ at 5 minutes post-injection and, eliminated through the urinary system within 2 hours post-injection. This study explores the promising developments in brain imaging facilitated by the [99mTc]-tricarbonyl histamine complex.
Keywords
Histamine ligand; Radiolabeled; [99mTc]-tricarbonyl core; bioevaluation; brain imaging

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