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

Table 4 Concentrations of roflumilast and zatolmilast in mouse plasma and brain tissues and the unbound brain-to-plasma partition coefficient (K_p,uu) values following oral administration (10 mg/kg) in mice

Parameter		Roflumilast	Zatolmilast
Concentration (ng/mL or ng/g at 4 h)	Plasma	30.6 ± 14.2	3627 ± 890
Concentration (ng/mL or ng/g at 4 h)	Brain	18.2 ± 12.9	1203 ± 345
Brain K_p		0.53	0.33
F_u (%)	Plasma	1.26 ± 0.58	0.26 ± 0.01
F_u (%)	Brain	0.37 ± 0.20	0.14 ± 0.02
Brain K_p,uu		0.17	0.18

Data are expressed as the mean ± standard deviation, n = 3. K_p, brain-to-plasma ratio; F_u, unbound drug fraction

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