Fig 1.
Original one-step radiosynthesis of [18F]T807(1).
Fig 2.
Improved two-step radiosynthesis of [18F]T807(1).
Fig 3.
Synthesis of precursor (3) and the non-radioactive standard (1a) of [18F]T807 (1).
Fig 4.
Modified TRACERLab FXFN module for [18F]T807 radiosynthesis.
Table 1.
Production and QC results of three consecutive productions of the [18F]T807 injection (n = 3).
Fig 5.
Representative semi-preparative HPLC chromatograms of [18F]T807 synthesized by Method A (on-line one-step t-Boc deprotection and HPLC purification, Waters HSS T3, 5 μm, 10 × 250 mm, 18% EtOH(pH 2.0, adjusted by HCl), 5.0 ml/min, 254 nm) (A) and Method B (two-step t-Boc deprotection and HPLC purification, Phenomenex Luna(2) HILIC, 5 μm, 10 × 250 mm, 0.1% HCl(aq), 254 nm, 3 mL/min) (B).
Fig 6.
Representative analytical radio-HPLC (A) and radio-TLC chromatograms (B) of [18F]T807 at 0, 2 and 4 hrs after EOS.
Table 2.
Stability of three consecutive productions of the [18F]T807 injection (n = 3).
Fig 7.
Representative whole-body biodistribution of [18F]T807 in normal mice at last time-frame post injection and non-decay-corrected time-activity curves of [18F]T807 in various organs of non-fasted mice (n = 4) and fasted mice (n = 3).
Fig 8.
Typical sagittal view of [18F]T807 whole-body images of a male Formosan Rock monkey at different time points (A) and Non-decay-corrected time-activity curves of [18F]T807 in various organs of monkeys (n = 2) (B).
Table 3.
Residence times (hr) of selected organs from the biodistribution data and microPET imaging of mice and monkeys.
Table 4.
Radiation dosimetry estimates of the [18F]T807 injection extrapolated from the mice and monkey biodistribution data.
Table 5.
Safety summary of the [18F]T807 injection.
Fig 9.
Representative axial PET images of [18F]T807 of an AD patient (male, age = 61, MMSE = 24).