Publikationsrepositorium - Helmholtz-Zentrum Dresden-Rossendorf

Novel indole radiotracers for 123I and 99Tcm labeling were designed. The corresponding reference compounds (Indole-I and Indole-MAMA-Re) and the precursor for 99Tcm labelling were synthesized. The compounds were characterized by IR, NMR, and MS analyses. 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 2) μmol/L, 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, 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.