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    123I和99Tcm标记的吲哚类σ2受体放射性示踪剂的设计、稳定化合物的合成及体外生物评价

    Design, Synthesis and in Vitro Biological Evaluation of Reference Compounds of 123I and 99Tcm Labeled Indole Radiotracers for

      摘要
    • 摘要: 设计了123I和99Tcm标记的吲哚类σ2受体肿瘤放射性示踪剂，合成了其稳定化合物 (IndoleI和Indole-MAMA-Re) 和标记前体(Indole-MAMA)。体外受体结合分析结果表明，化合物Indole-I对σ1和σ2受体的抑制常数Ki值分别为（0.574±0.355）μmol/L和（0.162±0.030）μmol/L(n=3)，Indole-MAMA-Re对σ1和σ2受体的抑制常数Ki值分别为（3.75±2.22）μmol/L和（7.83±4.87）μmol/L(n=3)。成功制备了99Tcm Indole-MAMA，纯化后经高效液相色谱法（HPLC）分析其放化纯大于90%。今后可在本文化合物的基础上通过结构优化，设计合成对σ2受体具有高亲和力和选择性的吲哚类SPECT肿瘤显像剂。

       

      Abstract: Novel indole radiotracers for 123I and 99Tcm labeling were designed. The corresponding reference compounds (Indole-I and Indole-MAMA-Re) and the precursor (Indole-MAMA) for 99Tcm labeling were synthesized. Competition binding assays in vitro show that the Ki values of Indole-I for σ1 and σ2 receptors are (0.574±0.355) μmol/L and (0.162±0.030) μmol/L( n =3), respectively. The Ki values of Indole-MAMA-Re for σ1 and σ2 receptors are (3.75±2.22) μmol/L and (7.83±4.87) μmol/L(n=3), respectively. Furthermore, 99Tcm Indole-MAMA was successfully prepared. The radiochemical purity (RCP) of 99Tcm-Indole-MAMA after purification was higher than 90% by HPLC analysis. The compounds reported in this paper may be used as lead compounds for further structural modification to develop indole SPECT tumor imaging agents with high affinity and selectivity for σ2 receptors.

       

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