Biodistribution of 99mTc–2-aminoestrone-3-methyl ether as a potential radiotracer for inflammation imaging
- 121 Downloads
Estrogens may have pro- and anti-inflammatory properties depending on the situation and the involved tissue. 2-Aminoestrone-3-methyl ether as an estrogenic derivative was prepared with a yield of 55 % and well characterized. 99mTc–2-aminoestrone-3-methyl ether radiotracer was synthesized to study its inflammatory binding specificity as a novel selective radiopharmaceutical for inflammation imaging. In-vivo biodistribution study of 99mTc–2-amino estrone-3-methyl ether complex in both bacterial infection and sterile inflammation showed high and rapid accumulation of 99mTc–2-aminoestrone-3-methyl ether complex at the site of sterile inflammation compared to bacterial infection sites (target-to-non target ratio equal to 4.12 ± 0.02). This high biological accumulation in inflamed cells suggests that 99mTc–2-aminoestrone-3-methyl ether complex may be suitable as a potential selective radiotracer able to image inflammatory sites.
KeywordsEstrone Technetium-99m Inflammation Imaging
This research project was supported by a grant from the “Research Center of Female Scientific and Medical Colleges”, Deanship of Scientific Research, King Saud University.
- 1.Yang M, Liu C, Niu M, Hu Y, Guo M, Zhang J, Luo Y, Yuan W, Yang M, Yun M, Guo L, Yan J, Liu D, Liu J, Jiang Y (2014) Phage-display library biopanning and bioinformatic analysis yielded a high-affinity peptide to inflamed vascular endothelium both in-vitro and in-vivo. J Controlled Release 174:72–80CrossRefGoogle Scholar
- 2.Zehnder P, Jenni W, Aeschlimann AG (1998) Systemic vasculitis and solid tumors (epitheliomas). Rev Rhum Engl Ed 65:442Google Scholar
- 3.Fain O (2002) Vasculitis and cancers. Rev Med Intern Found Soc Natl Fr Med Intern 23(Suppl. 5):551–553Google Scholar
- 11.Beltram J (1995) MR imaging of soft tissue infection. Magn Reson Imaging Clin N Am 3:743–751Google Scholar
- 20.Davis KE, Neinast MD, Sun K, Skiles WM, Bills JD, Zehr JA, Zeve D, Hahner LD, Cox DW, Gent LM, Xu Y, Wang ZV, Khan SA, Clegg DJ (2013) The sexually dimorphic role of adipose and adipocyte estrogen receptors in modulating adipose tissue expansion, inflammation, and fibrosis. Mol Metab 2:227–242CrossRefGoogle Scholar
- 24.Nayak TK, Hathaway HJ, Ramesh C, Arterburn JB, Dai D, Sklar LA, Norenberg JP, Prossnitz ER (2008) Preclinical development of a neutral, estrogen receptor–targeted, tridentate 99mTc(I)-estradiol-pyridin-2-yl hydrazine derivative for imaging of breast and endometrial cancers. J Nucl Med 49:978–986CrossRefGoogle Scholar