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A bisphosphonate for (19)F-magnetic resonance imaging.

Kenny GD, Shaw KP, Sivachelvam S, White AJ, Botnar RM, T M de Rosales R - J Fluor Chem (2016)

Bottom Line: The potential of (19)F-BP to provide contrast was analysed in vitro and in vivo using (19)F-MRI.The preliminary in vivo MRI study reported here allowed us to visualise the biodistribution of (19)F-BP, showing uptake in the liver and in the bladder/urinary system areas.However, bone uptake was not observed.

View Article: PubMed Central - PubMed

Affiliation: Division of Imaging Sciences & Biomedical Engineering, King's College London, St Thomas' Hospital, London SE1 7EH, UK.

ABSTRACT

(19)F-magnetic resonance imaging (MRI) is a promising technique that may allow us to measure the concentration of exogenous fluorinated imaging probes quantitatively in vivo. Here, we describe the synthesis and characterisation of a novel geminal bisphosphonate ((19)F-BP) that contains chemically-equivalent fluorine atoms that show a single and narrow (19)F resonance and a bisphosphonate group that may be used for labelling inorganic materials based in calcium phosphates and metal oxides. The potential of (19)F-BP to provide contrast was analysed in vitro and in vivo using (19)F-MRI. In vitro studies demonstrated the potential of (19)F-BP as an MRI contrast agent in the millimolar concentration range with signal-to-noise ratios (SNR) comparable to previously reported fluorinated probes. The preliminary in vivo MRI study reported here allowed us to visualise the biodistribution of (19)F-BP, showing uptake in the liver and in the bladder/urinary system areas. However, bone uptake was not observed. In addition, (19)F-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 developing (19)F MRI probes with the highest signal intensity achievable.

No MeSH data available.


Related in: MedlinePlus

In vitro MR imaging study. Top: 1H and 19F MRI phantom study with vials of 19F-BP at increasing concentrations (27, 54 and 108 mM) in water from left to right, with water above. Bottom: graph showing the increase of signal to noise ratio (SNR) with increasing probe concentration. The fit is a smooth curve fit intended to represent the trend. Error bars are the result of 3 ROI image analyses.
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fig0010: In vitro MR imaging study. Top: 1H and 19F MRI phantom study with vials of 19F-BP at increasing concentrations (27, 54 and 108 mM) in water from left to right, with water above. Bottom: graph showing the increase of signal to noise ratio (SNR) with increasing probe concentration. The fit is a smooth curve fit intended to represent the trend. Error bars are the result of 3 ROI image analyses.

Mentions: Phantom MRI studies were performed to evaluate the contrast properties of 19F-BP (Fig. 2). The compound was dissolved in water at pH 7 at several concentrations (27, 54 and 108 mM) and imaged in a preclinical 9.4 T MRI scanner. A clear concentration-dependent increase in signal intensity and signal to noise ratio (SNR) was found, demonstrating that 19F-BP can be imaged in the high mM concentration range. Stability studies were also performed using these samples. The 1H NMR and 19F-MRI spectra remained stable for 5 h at pH 7 and 37 °C, confirming the stability of 19F-BP at these conditions. This gave us confidence to study its biodistribution properties in vivo.


A bisphosphonate for (19)F-magnetic resonance imaging.

Kenny GD, Shaw KP, Sivachelvam S, White AJ, Botnar RM, T M de Rosales R - J Fluor Chem (2016)

In vitro MR imaging study. Top: 1H and 19F MRI phantom study with vials of 19F-BP at increasing concentrations (27, 54 and 108 mM) in water from left to right, with water above. Bottom: graph showing the increase of signal to noise ratio (SNR) with increasing probe concentration. The fit is a smooth curve fit intended to represent the trend. Error bars are the result of 3 ROI image analyses.
© Copyright Policy - CC BY
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4834630&req=5

fig0010: In vitro MR imaging study. Top: 1H and 19F MRI phantom study with vials of 19F-BP at increasing concentrations (27, 54 and 108 mM) in water from left to right, with water above. Bottom: graph showing the increase of signal to noise ratio (SNR) with increasing probe concentration. The fit is a smooth curve fit intended to represent the trend. Error bars are the result of 3 ROI image analyses.
Mentions: Phantom MRI studies were performed to evaluate the contrast properties of 19F-BP (Fig. 2). The compound was dissolved in water at pH 7 at several concentrations (27, 54 and 108 mM) and imaged in a preclinical 9.4 T MRI scanner. A clear concentration-dependent increase in signal intensity and signal to noise ratio (SNR) was found, demonstrating that 19F-BP can be imaged in the high mM concentration range. Stability studies were also performed using these samples. The 1H NMR and 19F-MRI spectra remained stable for 5 h at pH 7 and 37 °C, confirming the stability of 19F-BP at these conditions. This gave us confidence to study its biodistribution properties in vivo.

Bottom Line: The potential of (19)F-BP to provide contrast was analysed in vitro and in vivo using (19)F-MRI.The preliminary in vivo MRI study reported here allowed us to visualise the biodistribution of (19)F-BP, showing uptake in the liver and in the bladder/urinary system areas.However, bone uptake was not observed.

View Article: PubMed Central - PubMed

Affiliation: Division of Imaging Sciences & Biomedical Engineering, King's College London, St Thomas' Hospital, London SE1 7EH, UK.

ABSTRACT

(19)F-magnetic resonance imaging (MRI) is a promising technique that may allow us to measure the concentration of exogenous fluorinated imaging probes quantitatively in vivo. Here, we describe the synthesis and characterisation of a novel geminal bisphosphonate ((19)F-BP) that contains chemically-equivalent fluorine atoms that show a single and narrow (19)F resonance and a bisphosphonate group that may be used for labelling inorganic materials based in calcium phosphates and metal oxides. The potential of (19)F-BP to provide contrast was analysed in vitro and in vivo using (19)F-MRI. In vitro studies demonstrated the potential of (19)F-BP as an MRI contrast agent in the millimolar concentration range with signal-to-noise ratios (SNR) comparable to previously reported fluorinated probes. The preliminary in vivo MRI study reported here allowed us to visualise the biodistribution of (19)F-BP, showing uptake in the liver and in the bladder/urinary system areas. However, bone uptake was not observed. In addition, (19)F-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 developing (19)F MRI probes with the highest signal intensity achievable.

No MeSH data available.


Related in: MedlinePlus