| Literature DB >> 21146995 |
Takeshi Kuboyama1, Motoi Nakahara, Masafumi Yoshino, Yilong Cui, Takeo Sako, Yasuhiro Wada, Takeshi Imanishi, Satoshi Obika, Yasuyoshi Watanabe, Masaaki Suzuki, Hisashi Doi.
Abstract
A novel method for (18)F-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([(18)F]fluoromethyl)benzene and alkyne-substituted ODN (20nmol) at 40°C for 15min in the presence of CuSO(4), TBTA [tris((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)amine], and sodium ascorbate (2:1:2), the synthesis of (18)F-labeled ODNs with sufficiently high radioactivities of 2.1-2.5GBq and specific radioactivities of 1800-2400GBq/μmol have been accomplished for use in animal and human PET studies. Copyright ÂEntities:
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Year: 2010 PMID： 21146995 DOI： 10.1016/j.bmc.2010.11.033
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641