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F-19: A versatile reporter for non-invasive physiology and pharmacology using magnetic resonance

Journal

CURRENT MEDICINAL CHEMISTRY
Volume 12, Issue 7, Pages 819-848

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/0929867053507342

Keywords

oxygen; pH; gene reporter; metal ions; 5FU; FDG; anesthetics

Funding

  1. NATIONAL CANCER INSTITUTE [P20CA086354] Funding Source: NIH RePORTER
  2. NATIONAL CENTER FOR RESEARCH RESOURCES [P41RR002584] Funding Source: NIH RePORTER
  3. NCI NIH HHS [P20 CA086354, P20 CA0886354] Funding Source: Medline
  4. NCRR NIH HHS [P41-RR02584, P41 RR002584] Funding Source: Medline

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The fluorine atom provides an exciting tool for diverse spectroscopic and imaging applications using Magnetic Resonance. The organic chemistry Of fluorine is widely established and it can provide a stable moiety for interrogating many aspects of physiology and pharmacology in vivo. Strong NMR signal, minimal background signal and exquisite sensitivity to changes in the microenvironment have been exploited to design and apply diverse reporter molecules. Classes of agents are presented to investigate gene activity, pH, metal ion concentrations (e.g., Ca2+, Mg2+, Na+), oxygen tension, hypoxia, vascular flow and vascular Volume. In addition to interrogating speciality reporter molecules. F-19 NMR may be used to trace the fate of fluorinated drugs, such as chemotherapeutics (e.g., 5-fluorouracil, gemcitabine), anesthetics (e.g., isoflurane, methoxyflurane) and neuroleptics. NMR can provide useful information through multiple parameters, including chemical shift, scalar coupling, chemical exchange and relaxation processes (R1 and R2). Indeed, the large chemical shift range (similar to 300 ppm) can allow multiple agents to be examined, simultaneously, using NMR spectroscopy or chemical shift selective imaging.

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