In vitro characterization of pralidoxime transport and acetylcholinesterase reactivation across MDCK cells and stem cell-derived human brain microvascular endothelial cells (BC1-hBMECs)

Table 1 Permeability of pralidoxime (2-PAM), rhodamine 123 R123) and Lucifer yellow (Ly) across MDCKII, MDCKII-MDR1, MDCKII-FLuc-ABCG2, and BC1-hBMEC monolayers

	P_app A→B (cm s⁻¹)	N	P_app B→A (cm s⁻¹)	N	Efflux ratio
100 µM 2-PAM
MDCKII	2.99 ± 1.12 × 10⁻⁶	11	2.48 ± 1.30 × 10⁻⁶	8	0.82
MDCKII-MDR1	3.01 ± 1.27 × 10⁻⁶	8	2.51 ± 1.08 × 10⁻⁶	7	0.83
MDCKII-FLuc-ABCG2	0.76 ± 0.05 × 10⁻⁶	7	0.98 ± 0.40 × 10⁻⁶	7	1.30
BC1-hBMECs	1.12 ± 0.80 × 10⁻⁶ (n = 5)	18	0.49 ± 0.16 × 10⁻⁶ (n = 3)	12	0.84
10 µM 2-PAM
MDCKII	1.62 ± 0.21 × 10⁻⁶	6	1.29 ± 1.76 × 10⁻⁶	7	0.80
MDCKII-MDR1	2.03 ± 0.14 × 10⁻⁶	8	1.18 ± 0.45 × 10⁻⁶	8	0.58
MDCKII-FLuc-ABCG2	0.83 ± 0.35 × 10⁻⁶	7	0.99 ± 0.62 × 10⁻⁶	7	1.18
50 µM R123
MDCKII	0.30 ± 0.20 × 10⁻⁶	6	3.18 ± 0.60 × 10⁻⁶	5	10.7
MDCKII-MDR1	0.21 ± 0.21 × 10⁻⁶	12	4.36 ± 0.41 × 10⁻⁶	11	20.3
100 µM LY
MDCKII	0.71 ± 0.34 × 10⁻⁶	7
MDCKII-MDR1	0.38 ± 0.20 × 10⁻⁶	7
MDCKII-FLuc-ABCG2	0.46 ± 0.21 × 10⁻⁶	8
2-PAM atropine
MDCKII	2.54 ± 0.33 × 10⁻⁶	7

A→B represents apical-to-basolateral permeability, and B→A represents basolateral-to-apical permeability. Permeability values are reported as mean ± standard deviation. The efflux ratio is the ratio of basolateral-to-apical permeability divided by the apical-to-basolateral permeability. For MDCK cells, permeabilities and efflux ratios were calculated from the total number of replicates (N). Data were obtained from at least three independent experiments each with two or more replicates. For the BC1-hBMECs, the permeabilities and efflux ratios were calculated from the average of each differentiation, where N represents the number of independent differentiations

ISSN: 2045-8118