期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 -, 期 -, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202219181
关键词
Dissolution-DNP; Hyperpolarization; Imaging Agents; NMR Spectroscopy; Nitrogen-15
We present the first report of dissolution Dynamic Nuclear Polarization (d-DNP) of [N-15(3)]metronidazole ([N-15(3)]MNZ). Metronidazole, a clinically approved antibiotic, shows potential as a hypoxia-sensing molecular probe using N-15 hyperpolarized (HP) nucleus. The d-DNP process using trityl radical achieves efficient hyperpolarization of [N-15(3)]MNZ with long-lasting signal and high polarization.
We report dissolution Dynamic Nuclear Polarization (d-DNP) of [N-15(3)]metronidazole ([N-15(3)]MNZ) for the first time. Metronidazole is a clinically approved antibiotic, which can be potentially employed as a hypoxia-sensing molecular probe using N-15 hyperpolarized (HP) nucleus. The DNP process is very efficient for [N-15(3)]MNZ with an exponential build-up constant of 13.8 min using trityl radical. After dissolution and sample transfer to a nearby 4.7 T Magnetic Resonance Imaging scanner, HP [N-15(3)]MNZ lasted remarkably long with T-1 values up to 343 s and N-15 polarizations up to 6.4 %. A time series of HP [N-15(3)]MNZ images was acquired in vitro using a steady state free precession sequence on the (NO2)-N-15 peak. The signal lasted over 13 min with notably long T-2 of 20.5 s. HP [N-15(3)]MNZ was injected in the tail vein of a healthy rat, and dynamic spectroscopy was performed over the rat brain. The in vivo HP N-15 signals persisted over 70 s, demonstrating an unprecedented opportunity for in vivo studies.
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