Matrix | Analyte | Concentrationa | Unbound fractionb |
---|---|---|---|
Plasma | TREO | 2.3 μM | 0.962 ± 0.137 |
57 μM | 0.940 ± 0.061 | ||
2000 μM | 0.960 ± 0.163 | ||
S,S-EBDM | 3.5 μM | 1.083 ± 0.211 | |
87 μM | 0.986 ± 0.119 | ||
Brain homogenate | TREO | 2.3 μM | 1.063 ± 0.172 |
5.7 μM | 0.999 ± 0.081 | ||
17.2 μM | 1.000 ± 0.108 | ||
S,S-EBDM | 3.5 μM | 1.092 ± 0.079 | |
8.7 μM | 0.974 ± 0.075 |
↵a The used concentrations covered the range observed in the JR and the YAR that received TREO 500 mg/kg b.wt. as an intravenous bolus.
↵b At each concentration level of TREO or S,S-EBDM the unbound fraction was determined using five lots of plasma and brain homogenate obtained from different 2-mo-old rat donors.