TABLE 1

Bidirectional P_app coefficient, ER, and net flux ratio of reference compounds across MDCK II, MDCK-MDR1, and MDCK-BCRP cell monolayers

The P_app values are indicated from the AP-BL and BL-AP compartments and are expressed as mean (S.D.) (n = 3). ERs and net flux ratios greater than 2 are marked in bold. Transport classification according to Mahar Doan et al. (2002), Pavek et al. (2005), Wang et al. (2005), Feng et al. (2008), and Urquhart et al. (2008).

Reference Compound	Transport	Donor Solution	MDCK II			MDCK-MDR1			Net Flux Ratio		MDCK-BCRP			Net Flux Ratio
Reference Compound	Transport	Donor Solution	P_app,AP-BL (×10⁻⁶)	P_app,BL-AP (×10⁻⁶)	ER	P_app,AP-BL (×10⁻⁶)	P_app,BL-AP (×10⁻⁶)	ER	Without Verapamil	With Verapamil	P_app,AP-BL (×10⁻⁶)	P_app,BL-AP (×10⁻⁶)	ER	Without Ko143	With Ko143
		μM	cm/s	cm/s		cm/s	cm/s				cm/s	cm/s
Carbamazepine	PT	10	36.5 (1.93)	19.5 (0.60)	0.53	38.0 (2.54)	20.0 (5.53)	0.53	1.00	—	37.3 (5.60)	19.6 (3.85)	0.53	1.00	—
Propranolol	PT	10	19.6 (4.99)	20.0 (0.16)	1.02	23.8 (2.69)	20.8 (1.51)	0.87	0.85	—	25.4 (2.51)	22.4 (0.59)	0.88	0.86	—
Trazodone	PT	10	38.5 (3.30)	29.4 (1.31)	0.76	33.0 (2.58)	40.4 (3.14)	1.22	1.61	—	37.5 (5.03)	27.4 (2.91)	0.73	0.96	—
Atenolol	PP	100	0.22 (0.06)	0.28 (0.03)	1.27	0.35 (0.14)	0.24 (0.04)	0.69	0.54	—	0.14 (0.11)	0.20 (0.03)	1.43	1.13	—
Cimetidine	Efflux^{^a}	30	0.56 (0.14)	0.43 (0.03)	0.75	0.06 (0.02)	0.41 (0.05)	6.40	8.50	0.89	0.15 (0.04)	1.25 (0.08)	8.34	11.1	1.47
Quinidine	Efflux^{^b}	10	9.52 (2.53)	12.5 (2.49)	1.31	3.77 (0.91)	29.1 (1.37)	7.73	5.90	1.13	12.0 (3.48)	15.0 (0.48)	1.25	0.95	—
Sulfasalazine	Efflux^c	60	0.81 (0.30)	0.28 (0.05)	0.34	0.30 (0.14)	0.17 (0.09)	0.56	1.64	—	0.13 (0.11)	0.30 (0.05)	2.31	6.79	0.92
Na-F	PP	100	0.48 (0.09)	—	—	0.09 (0.08)	—	—	—	—	0.11 (0.04)	—	—	—	—

PP, passive paracellular; PT, passive transcellular.
↵^a Efflux mediated by P-gp and BCRP.
↵^b Efflux mediated by P-gp.
↵^c Efflux mediated by BCRP.