A bisphosphonate for19F-magnetic resonance imaging.
19F-magnetic resonance imaging (MRI) is a promising technique that may allow us to measure the concentration of exogenous fluorinated imaging probes quantitativelyin vivo.Here, we describe the synthesis and characterisation of a novel geminal bisphosphonate (19F-BP) that contains chemically-equivalent fluorine atoms that show a single and narrow19F resonance and a bisphosphonate group that may be used for labelling inorganic materials based in calcium phosphates and metal oxides. The potential of19F-BP to provide contrast was analysedin vitroandin vivousing19F-MRI. In vitrostudies demonstrated the potential of19F-BP as an MRI contrast agent in the millimolar concentration range with signal-to-noise ratios (SNR) comparable to previously reported fluorinated probes. The preliminaryin vivoMRI study reported here allowed us to visualise the biodistribution of19F-BP, showing uptake in the liver and in the bladder/urinary system areas. However, bone uptake was not observed. In addition,19F-BP showed undesirable toxicity effects in mice that prevent further studies with this compound at the required concentrations for MRI contrast. This study highlights the importance of developing19F MRI probes with the highest signal intensity achievable.
Division of Imaging Sciences & Biomedical Engineering, King's College London, St Thomas' Hospital, London SE1 7EH, UK.
Gavin D
GD
Kenny
Division of Imaging Sciences & Biomedical Engineering, King's College London, St Thomas' Hospital, London SE1 7EH, UK.
Karen P
KP
Shaw
Division of Imaging Sciences & Biomedical Engineering, King's College London, St Thomas' Hospital, London SE1 7EH, UK.
Saranja
S
Sivachelvam
Department of Chemistry, Imperial College London, Exhibition Road, South Kensington, London SW7 2AZ, UK.
Andrew J P
AJ
White
Division of Imaging Sciences & Biomedical Engineering, King's College London, St Thomas' Hospital, London SE1 7EH, UK.
Rene M
RM
Botnar
Division of Imaging Sciences & Biomedical Engineering, King's College London, St Thomas' Hospital, London SE1 7EH, UK.
Rafael
R
T M de Rosales
19F-MRI; Bisphosphonates (BPs); Fluorinated bisphosphonate; Magnetic resonance imaging (MRI); Preclinical imaging