Figure 2 | Scientific Reports

Figure 2

From: Discovery of a brain penetrant small molecule antagonist targeting LPA1 receptors to reduce neuroinflammation and promote remyelination in multiple sclerosis

Figure 2

PIPE-791 has distinct in vivo brain occupancy kinetics. (A) Dose-occupancy was assessed 2 h or 24 h after administration of PIPE-791. For the steady state condition, mice were dosed once daily for 4 days then occupancy assessed 2 h after the fourth dose (mean ± SEM, n = 6). (B) Pooled analysis of unbound brain concentration (Cu, brain) plotted versus occupancy. (C) Time course of 3 mg/kg PIPE-791 plotted against brain receptor occupancy (left y-axis) and plasma concentration (right y-axis) highlighting its extended brain receptor occupancy and disconnect with plasma concentration (mean ± SEM, n = 6).

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