本研究主要目的是在合成TTDA-PSA。TTDA-PSA的合成主要是合成出TTDA-NCS與具有攝護腺癌目標化胜肽PSA反應,而得到目標化對比劑TTDA-PSA。之所以會選用TTDA-NCS當配位子的主要理由是,因本實驗室先前研究發現[Gd(TTDA-NP)]2-,具有較高之穩定常數,與較佳之水交換速率,所以具有其較好之弛緩(r1)。因此用它來推測其衍生物TTDA-NCS也應具有相同特質,而且可以藉由結合PSA而降低分子轉動時間,進而達到更高弛緩率。此外,本研究也針對影響PSA與TTDA-NCS的結合因素作一探討,探討其:(1)pH值,(2)立體障礙,(3)反應物純度與(4)反應物當量比,以期能夠找出合成TTDA-PSA的最佳化條件,以便在未來的研究上,可以得到較高之產率。
Synthesis and Application study of TTDA-PSA is the goal of this thesis. The reaction of TTDA-NCS with prostate cancer targeting peptide PSA(Prostate Specific Antigen) will afford a targeting contrast agent TTDA-PSA. Since our laboratory had studied the application of [Gd(TTDA-NP)]2-, which has stability and excellent water exchange rate(kex298) value for contrast agent. Therefore, the TTDA-NCS may have similar stability and excellent water exchange rate(kex298) value in it’s Gd complex for contrast agent. The synthesis of TTDA-PSA will affect and control in four factors: (1) pH value, (2) steric effect, (3) purity of reactant, (4) equivalent amount of reactant. The best reaction condition are discussed in this study.