Species (Strain) | BCRP Expression at BBB | ERin vivo of Dantrolene | Predicted Kp,uua | Reference |
---|---|---|---|---|
fmol/μg⋅protein | ||||
Mouse (Friend virus B) | 3.53, 3.21 (mean 3.37) | 6.30 | 0.16 | Enokizono et al. (2008); Uchida et al. (2013);Agarwal et al. (2012) |
Rat (Sprague Dawley) | 4.15 | 3.30 | 0.30 | Hoshi et al. (2013); Fuchs et al. (2014) |
Human | 6.15, 8.14 (mean 7.15) | 9.1 (predicted)b | 0.10 | Shawahna et al. (2011); Uchida et al. (2011b) |
↵a The Kp,uu value was predicted by the reciprocal of the ERin vivo value (eq. 6).
↵b The human ERin vivo value of dantrolene was predicted by (mean ERin vivo of dantrolene in mouse and rat −1) ÷ ratio of mean BCRP expression at mouse and rat to human BBB + 1. The BCRP transport capacity was assumed to be the same in human as mouse and rat.