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摘要
Introduction: Tc-99m compounds are mainly used in myocardial blood flow studies. These compounds, however, are produced by a generator and alternate single photon emission computed tomography (SPECT) radiopharmaceuticals are therefore required to avoid the risks posed by generator failure. Three radiolabeled compounds, including [I-125]p-iodobenzyl triphenylphosphonium ([I-125]ITPP), [I-125]p-lodobenzyl dipropylphenylphosphonium ([I-125]IDPP) and [I-125]p-iodobenzyl methyldiphenylphosphonium ([I-125]IMPP), have been synthesized in the current study. All three of these compounds contain a lipophilic cation, which enhances their cell permeability properties and allows them to accumulate in the myocardium as SPECT probes. Methods: 4-(2-Tributylstannyl) benzyl alcohol was mixed with [I-125]NaI in the presence of aqueous hydrogen peroxide and hydrochloric acid to allow for the synthesis of 4-[I-125]iodobenzyl alcohol. Bromination of the alcohol under standard conditions gave 4-[I-125]iodo benzyl bromide, which was treated with triphenylphosphine, dipropylphenylphosphine or methyldiphenylphosphine to give [I-125]ITPP, [I-125]IDPP and [I-125]IMPP, respectively. These compounds were evaluated in biodistribution and SPECT studies in normal ddY mice. Results: All three of the radiolabeled compounds were synthesized in approximately 60% yield with radiochemical purities greater than 99%. The specific activity of each compound was 74 GBq/mu mol. The results of the biodistribution and SPECT studies showed that all compounds accumulated preferentially in the heart in vivo, especially [I-125]IDPP. Conclusion: [I-123] IDPP could be used in clinical practice as a novel myocardial imaging agent.
- 出版日期2015-5
