Route Dose Level (mmol/kg) C0a (µg/mL) (Cmax for po) tmax (h) AUCb (h•µg/mL) Cl (mL/h/kg)c V (L/kg)c t½ (h) Fd(%)
5-LIO(Me-3,2-HOPO)
iv 100 197 ± 6 NAe 107 ± 9 383 ± 30 0.42 ± 0.06 0.77 ± 0.06 NA
po 150 7.12 ± 4.90 0.50 ± 0.00 8.27 ± 5.41 380 ± 1 0.47 ± 0.11 0.85 ± 0.21 5.15 ± 3.38
po 500 9.07 ± 7.98 0.83 ± 0.29 17.0 ± 16.4 381 ± 2 1.00 ± 0.12 1.83 ± 0.23 3.19 ± 3.07
3,4,3-LI(1,2-HOPO)
iv 30 144 ± 27 NA 47 ± 6 481 ± 63 1.60 ± 0.23 2.33 ± 0.44 NA
po 100 NDf ND ND ND ND ND ND
po 500 1.77 ± 0.64 1.25 ± 1.52 3.79 ± 1.03 479 ± 3 0.78 ± 0.46 1.13 ± 0.66 0.48 ± 0.13
aC0 is the plasma concentration extrapolated to time zero.
bAUC presented is extrapolated to infinity.
cFor po administrations, V and Cl were calculated from V/F•F and Cl/F•F, respectively.
dThe bioavailability F is expressed as a percentage.
eNA = not applicable.
fND = no data, the test article was not detected.
Table 1: Mean pharmacokinetic parameters of 5-LIO(Me-3,2-HOPO) and 3,4,3-LI(1,2-HOPO) in male Sprague-Dawley rats (n = 3).