In Vivo Microdialysis | In Vitro Brain Slice Uptake (n = 5-7) | In Vitro Brain Homogenate Binding (n = 3) | Predicted from Log D7.4 | ||
---|---|---|---|---|---|
Alovudine (A)a,b,c | (Linden et al., 2003) | 0.52d | 1.07 ± 0.091 | 1.05 ± 0.30 | 0.66 |
R-Apomorphine (R-A)c,e | (Sam et al., 1997) | 15d | 18.1 ± 1.9 | 15.5 ± 0.38 | 16.8 |
S-Apomorphine (S-A)c,e | (Sam et al., 1997) | 26d | 14.0 ± 1.4 | 14.4 ± 0.76 | 15.5 |
R-Cetirizine (R-C)b,c,f,g | (Gupta et al., 2006) | 2.39h | 6.62 ± 0.56 | 11.8 ± 0.80 | 5.99 |
S-Cetirizine (S-C)b,c,f,g | (Gupta et al., 2006) | 2.86h | 6.56 ± 0.61 | 11.8 ± 0.80 | 4.90 |
Codeine (C)i | (Xie and Hammarlund-Udenaes, 1998) | 3.6 ± 1.2h | 2.77 ± 0.22 | 1.46 ± 0.18 | 1.41 |
CP-122721 (CP)c | 207 ± 14j | 210 ± 17 | 152 ± 19 | 21.3 | |
Diazepam (D)k,l | (Dubey et al., 1989) | 22d | 17.7 ± 0.80 | 24.6 ± 1.2 | 28.1 |
Gabapentin (G)c | (Wang and Welty, 1996) | 5.5 ± 2.0h | 3.97 ± 0.77m | 1.04 ± 0.14 | 0.27 |
Morphine (M)c | (Tunblad et al., 2003) | 1.7h | 2.69 ± 0.43 | 2.00 ± 0.20 | 0.67 |
Morphine-3-glucuronide (M3G)c | (Xie et al., 2000) | 0.25 ± 0.02h | 0.528 ± 0.059 | 1.27 ± 0.18 | 0.36 |
Morphine-6-glucuronide (M6G)c | (Bouw et al., 2001) | 0.20 ± 0.02h | 0.731 ± 0.078 | 1.24 ± 0.10 | 0.57 |
Norfloxacin (N)n,o | (Ooie et al., 1997) | 0.98 ± 0.59h | 2.01 ± 0.10 | 1.72 ± 0.37 | 0.31 |
Oxycodone (O)i | (Bostrom et al., 2006) | 2.20 ± 0.53h | 3.60 ± 0.35 | 1.95 ± 0.33 | 4.60 |
Thiopental (T)p | (Mather et al., 2000) | 10d | 5.07 ± 0.29 | 6.51 ± 0.89 | 34.8 |
↵ a Drug administration by subcutaneous bolus dose.
↵ b Estimation of Vu,brain during non-steady-state conditions.
↵ c Probe calibration by in vivo retrodialysis by drug.
↵ d Vu,brain calculated from data in original literature report.
↵ e Drug administration by continuous subcutaneous infusion.
↵ f Experiments performed in guinea pigs.
↵ g Drug administration by short intravenous infusion.
↵ h Vu,brain reported in original literature.
↵ i Probe calibration by in vivo retrodialysis by calibrator.
↵ j Vu,brain experimentally obtained from original data in this study.
↵ k Probe calibration in vitro.
↵ l Probe placement in cortex.
↵ m Vu,brain calculated from slices incubated for 1 h.
↵ n Probe calibration in vivo by reference compound.
↵ o Probe placement in hippocampus.
↵ p Probe calibration by in vivo retrodialysis by drug and correction.