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양전자 방출핵종 68Ga을 이용한 NOTA와 DOTA의 표지 및 시험관내 특성 연구
Radiolabeling of NOTA and DOTA with Positron Emitting 68Ga and

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Authors
Jeong, Jae Min; Kim, Young Ju; Lee, Yun-Sang; Lee, Dong Soo; Chung, June-Key; Lee, Myung Chul
Issue Date
2009
Publisher
대한핵의학회 = The Korean Society of Nuclear Medicine
Citation
Nucl Med Mol Imaging 2009;43(4):330-336
Keywords
Ga-68galliumprotein bindingbifunctional chelating agentgeneratorNOTADOTA
Abstract
Purpose: We established radiolabeling conditions of NOTA and DOTA with a generator-produced PET radionuclide
68Ga and studied in vitro characteristics such as stability, serum protein binding, octanol/water distribution, and
interference with other metal ions. Materials and Methods: Various concentrations of NOTA․3HCl and DOTA․
4HCl were labeled with 1 mL 68GaCl3 (0.18~5.75 mCi in 0.1 M HCl) in various pH. NOTA․3HCl (0.373 mM) was
labeled with 68GaCl3 (0.183~0.232 mCi/0.1 M HCl 1.0 mL) in the presense of CuCl2, FeCl2, InCl3, FeCl3, GaCl3, MgCl2
or CaCl2 (0~6.07 mM) at room temperature. The labeling efficiencies of 68Ga-NOTA and 68Ga-DOTA were checked
by ITLC-SG using acetone or saline as mobile phase. Stabilities, protein bindings, and octanol distribution
coefficients of the labeled compounds also were investigated. Results: 68Ga-NOTA and 68Ga-DOTA were labeled
optimally at pH 6.5 and pH 3.5, respectively, and the chelates were stable for 4 hr either in the reaction mixture
at room temperature or in the human serum at 37°C. NOTA was labeled at room temperature while DOTA
required heating for labeling. 68Ga-NOTA labeling efficiency was reduced by CuCl2, FeCl2, InCl2, FeCl3 or GaCl3,
however, was not influenced by MgCl2 or CaCl2. The protein binding was low (2.04~3.32%). Log P value of
68Ga-NOTA was -3.07 indicating high hydrophilicity. Conclusion: We found that NOTA is a better bifunctional
chelating agent than DOTA for 68Ga labeling. Although, 68Ga-NOTA labeling is interfered by various metal ions, it
shows high stability and low serum protein binding.
ISSN
1975-129X
Language
Korean
URI
http://ksnm.or.kr/journal/view.php?year=2009&vol=43&no=4&startpage=330

https://hdl.handle.net/10371/21270
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