OtherBasic Science Investigations

Radiopharmaceutical Chemistry of Targeted Radiotherapeutics, Part 2: Radiolytic Effects of 211At α-Particles Influence N-Succinimidyl 3-211At-Astatobenzoate Synthesis

Oscar R. Pozzi and Michael R. Zalutsky
Journal of Nuclear Medicine August 2005, 46 (8) 1393-1400;

Article Figures & Data

Figures

  • FIGURE 1.
    FIGURE 1.

    Normal-phase HPLC profile of radioactive species present after exposure of BuSTB precursor to 211At at doses of 644, 1,658, and 4,157 Gy and acetic acid in chloroform. Arrow indicates retention time of SIB standard. Chromatograms are offset on both axes for display purposes.

  • FIGURE 2.
    FIGURE 2.

    Reverse-phase HPLC profile of radioactive species present after exposure of MeSTB precursor to 211At at doses of 1,254, 3,252, and 6,724 Gy and acetic acid in chloroform. Arrows indicate retention times of SIB and IBA standards. Chromatograms are offset on both axes for display purposes.

  • FIGURE 3.
    FIGURE 3.

    Production of SAB after incubation of BuSTB and MeSTB with chloroform, acetic acid, and 211At as function of radiation dose.

  • FIGURE 4.
    FIGURE 4.

    Effect of sample evaporation on HPLC profile. Shown are chromatograms from reverse-phase HPLC analyses of radioactive species in samples from reaction of MeSTB with methanol, acetic acid, and 211At for reaction mixtures receiving doses of 1,873 Gy (evaporated) and 1,540 Gy (nonevaporated). Arrow indicates SAB.

  • FIGURE 5.
    FIGURE 5.

    Production of SAB after incubation of BuSTB and MeSTB with methanol, acetic acid, and 211At as function of radiation dose. Error bars indicate SDs.

  • FIGURE 6.
    FIGURE 6.

    Production of SAB from reaction of BuSTB and 211At with methanol and acetic acid by radiolysis (no oxidant added) and radiosynthesis (oxidant added). Decomposition of BuSTB as function of radiation dose (1) is shown for comparison.

  • FIGURE 7.
    FIGURE 7.

    Effect of addition of acetic acid on SAB synthesis from BuSTB in methanol as function of radiation dose. Error bars indicate SDs.

  • FIGURE 8.
    FIGURE 8.

    Reverse-phase HPLC profile of radioactive species present after exposure of MeSTB precursor to 211At at doses of 1,900 and 5,316 Gy in benzene and acetic acid. Arrows indicate retention times of MeSTB, SIB, and IBA standards.

  • FIGURE 9.
    FIGURE 9.

    Calculated micromoles of hydrogen and formaldehyde produced in methanol by radiolysis during 20-min reaction period as function of radiation dose. For comparison, broken line shows micromoles of oxidant (NCS) added to SAB radiosynthesis reaction.

Tables

  • TABLE 1

    Percentages of Activity Eluted at 18–23 Minutes in Benzene

    PrecursorDose (Gy)% Activity
    MeSTB1,90095
    5,12591
    5,31691
    12,46489
    BuSTB6,98882
    14,58297
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