Differential effects of two phosphodiesterase 4 inhibitors against lipopolysaccharide-induced neuroinflammation in mice

Table 1 Apparent permeability coefficients (P_app) and efflux ratios for roflumilast and zatolmilast (3, 10, and 30 µM) using the MDR1-MDCK monolayer assay

Compound	Concentration (µM)	P_app (× 10^–6 cm/s)		ER
Compound	Concentration (µM)	Apical → Basolateral	Basolateral → Apical	ER
Roflumilast	3	25.1 ± 1.28	23.9 ± 3.61	0.95
	10	44.5 ± 2.53 ^***	40.8 ± 6.48 ^#	0.91
	30	113 ± 5.70 ^***	72.2 ± 6.32 ^###	0.64
Zatolmilast	3	3.72 ± 0.33	7.18 ± 1.53	1.92
	10	9.59 ± 0.84 ^***	18.0 ± 1.37 ^###	1.89
	30	70.3 ± 9.58 ^***	126 ± 8.39 ^###	1.81

Data are expressed as the mean ± standard deviation, n = 3. ^***P < 0.001 versus the apical-to-basolateral value at 3 µM; ^#P < 0.05, ^###P < 0.001 versus the basolateral-to-apical value at 3 µM

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