TABLE 2

Transwell assays using MDR1-MDCK, Mdr1a-MDCK, and MDCK cells, ATPase assay, calcein AM P-gp inhibition assay, and B/P AUC ratios in Mdr1a/1b (-/-, -/-) and FVB mice for 7 non-CNS drugs

Boldface indicates positive efflux.

Drugs
B/P in KO/WTa
MDR1-MDCK Efflux Ratiob
Mdr1a-MDCK Efflux Ratiob
MDCK Efflux Ratiob
Ratio of Ratios in MDR1-MDCK/MDCK
Ratio of Ratios in Mdr1a-MDCK/MDCK
ATPase Kmb
Calcein IC50
μM μM
Loperamide 9.3* 9.4 ± 4.08 7.1 ± 2.70 2.5 ± 1.31 3.8 2.9 11.4 ± 0.22 4.9
Loratadine 1.9 0.9 ± 0.35 1.0 ± 0.46 1.8 ± 1.18 0.5 0.6 1.4 ± 0.90 7.5
Prazosin 2.0 3.2 ± 0.61 3.3 ± 0.77 1.1 ± 0.22 2.9 3.1 54.6 ± 3.00 >100
Prednisone 2.3 3.8 ± 0.88 3.4 ± 0.74 1.3 ± 0.34 2.8 2.5 291 ± 9.9 >100
Quinidine 36* 16.1 ± 4.40 14.3 ± 5.25 2.2 ± 0.65 7.4 6.6 13.7 ± 2.71 30.2
Ritonavir 1.2 49.5 ± 29.65 64.4 ± 21.5 2.7 ± 0.20 18.4 23.9 11.3 ± 1.16 63.5
Verapamil
17*
1.8 ± 0.10
1.2 ± 0.22
0.8 ± 0.20
2.1
1.4
9.0 ± 0.38
18.1

  • ↵* P < 0.05, probability of KO/WT ratio > 4.

  • ↵ a The data for B/P in P-gp KO/WT mice were extracted from Doran et al. (2005).

  • ↵ b Data are presented as mean ± S.D.