19F-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 (19F-BP) that contains chemically-equivalent fluorine atoms that show a single and narrow 19F resonance and a bisphosphonate group that may be used for labelling inorganic materials based in calcium phosphates and metal oxides. The potential of 19F-BP to provide contrast was analysed in vitro and in vivo using 19F-MRI. In vitro studies demonstrated the potential of 19F-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 19F-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 developing 19F MRI probes with the highest signal intensity achievable.

中文翻译：

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用于 19F 磁共振成像的双膦酸盐。

19F-磁共振成像（MRI）是一种很有前途的技术，它可以让我们定量测量体内外源性氟化成像探针的浓度。在这里，我们描述了一种新型偕双膦酸盐 (19F-BP) 的合成和表征，该双膦酸盐含有化学等效的氟原子，显示出单一且窄的 19F 共振，以及可用于标记基于磷酸钙的无机材料和双膦酸盐基团。金属氧化物。使用 19F-MRI 在体外和体内分析 19F-BP 提供对比的潜力。体外研究证明了 19F-BP 在毫摩尔浓度范围内作为 MRI 造影剂的潜力，其信噪比 (SNR) 与之前报道的氟化探针相当。这里报道的初步体内 MRI 研究使我们能够可视化 19F-BP 的生物分布，显示肝脏和膀胱/泌尿系统区域的吸收。然而，没有观察到骨摄取。此外，19F-BP 在小鼠中表现出不良毒性作用，这阻碍了在 MRI 对比所需浓度下对该化合物进行进一步研究。这项研究强调了开发具有最高信号强度的 19F MRI 探头的重要性。