Table 2.

Permeability coefficients (P_app) for selected drugs on the primary rat brain endothelial cell-based BBB model (EPA) and in epithelial cell line models (Caco-2, VB-Caco-2, MDCK and MDCK-MDR1) measured in the apical to basal (A-B) direction.

Ligands	SLC	EPA		Caco-2		VB-Caco-2		MDCK		MDCK-MDR1
		Papp A-B	PDR	Papp A-B	PDR	Papp A-B	PDR	Papp A-B	PDR	Papp A-B	PDR
Glucopyranose	GLUT1	<65.7	>0.14	57.83	0.64	17.17	1.17	<18.5	NA	<18.5	NA
Valproic acid	LAT1, OATPs	39.37	0.98	51.91	0.82	42.22	0.87	26.62	1.22	27.49	1.26
Baclofen	LAT1	16.34	0.85	1.23	0.77	0.31	0.47	1.28	0.77	0.68	0.82
Gabapentin	LAT1, Pgp, BCRP	2.98	0.92	1.80	0.77	<0.88	>0.27	3.35	0.28	4.75	0.42
Probenecid	MCT, OATs	18.96	0.79	27.34	0.88	33.39	0.88	19.37	0.83	17.23	0.98
Salicylic acid	MCT1, OATPs, MRP4	4.78	1.88	16.63	1.11	7.60	1.19	13.01	0.86	9.31	0.85
Rosuvastatin	OATPs, Pgp, MRP2, BCRP	11.31	0.80	0.92	9.41	0.38	12.80	0,.9	0.52	0.81	1.13
Pravastatin	OATPs, MRP2	7.61	1.14	1.50	0.90	0.19	0.80	0.58	2.40	0.30	1.09
Atorvastatin	OATPs, MCT, Pgp, MRP2, BCRP	3.93	1.44	7.53	1.28	2.98	4.34	2.36	1.09	1.66	5.76

BCRP, breast cancer resistance protein; GLUT1, glucose transporters; LAT1, large neutral amino acid transporter; MCT, monocarboxylic acid transporter; MRP, multidrug resistance-associated proteins; OAT, organic anion transporter; OATP, organic anion-transporting polypeptide; PDR, permeability directional ratio; Pgp, P glycoprotein.