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1975年R.J.Baker等已使用 ~(99m)Tc标记的吡哆醛氨基酸类作为肝胆显像剂,但其制备繁复且需高压程序。其后采用亚锡离子作还原剂,已能在常压下进行标记。1982年Kato-Azuma等将吡哆醛和氨基酸缩合形成的亚胺键(R_2C=N-R′)经加压加氢还原为稳定的胺键(R_2HC-NHR′)。这样形成的化合物更为稳定,易于制备药盒,并免除了药盒中需要大量吡哆醛和氨基酸的缺点及减少了与螯合剂竞争的潜在可能。我们参考有关文献在常温常压下成功地制备了吡哆色氨酸(PHT),化学名N-{[(3-羟基-5-羟甲基)-2-甲基-4-吡啶]甲基}-L-色氨酸。本文报道其合成、药盒制备、标记、动物实验和初步试用的结果。
In 1975, R.J. Baker et al. Have used ~ (99m) Tc-labeled pyridoxal amino acids as hepatobiliary imaging agents, but their preparation is complicated and requires high-pressure procedures. Subsequent use of stannous ions as reductant, has been able to mark at atmospheric pressure. In 1982, Kato-Azuma and other pyridoxal and amino acid condensation formed by the imine bond (R_2C = N-R ’) by pressurized hydrogenation to a stable amine bond (R_2HC-NHR’). The compounds thus formed are more stable, easy to prepare, and dispense with the drawbacks of requiring large amounts of pyridoxal and amino acids in the kit and reducing the potential for competition with chelators. We refer to the literature at room temperature and pressure successfully prepared pyridoxine (PHT), the chemical name N - {[(3-hydroxy-5-hydroxymethyl) -2- methyl-4-pyridine] A Yl} -L-tryptophan. This article reports the results of their synthesis, kit preparation, labeling, animal experiments and preliminary trials.