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Stoichiometry-focused (18)F-labeling of alkyne-substituted oligodeoxynucleotides using azido([(18)F]fluoromethyl)benzenes by Cu-catalyzed Huisgen reaction |
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| Authors: | Kuboyama Takeshi Nakahara Motoi Yoshino Masafumi Cui Yilong Sako Takeo Wada Yasuhiro Imanishi Takeshi Obika Satoshi Watanabe Yasuyoshi Suzuki Masaaki Doi Hisashi |
| Affiliation: | a Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamadaoka, Suita, Osaka 565-0871, Japan b RIKEN Center for Molecular Imaging Science, 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan c GeneDesign, Inc., 7-7-20 Saitoasagi, Ibaraki, Osaka 567-0085, Japan |
| Abstract: | A novel method for 18F-radiolabeling of oligodeoxynucleotides (ODNs) by a Cu-catalyzed Huisgen reaction has been developed by using the lowest possible amount of the precursor biomolecule for the realization of stoichiometry-oriented PET (positron emission tomography) chemistry. Under the optimized cyclization conditions of p- or m-azido([18F]fluoromethyl)benzene and alkyne-substituted ODN (20 nmol) at 40 °C for 15 min in the presence of CuSO4, TBTA [tris((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)amine], and sodium ascorbate (2:1:2), the synthesis of 18F-labeled ODNs with sufficiently high radioactivities of 2.1-2.5 GBq and specific radioactivities of 1800-2400 GBq/??mol have been accomplished for use in animal and human PET studies. |
| Keywords: | PET, positron emission tomography ODN, oligodeoxynucleotide SPE, solid phase extraction TBTA, tris((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)amine DCY, decay-corrected radiochemical yield DOTA, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid TEAA, triethylammonium acetate |
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