Fig. 3
Assessment of regional Kp and Kp, uu for eletriptan and sumatriptan in rats under steady state. A Schematic overview of the neuropharmacokinetic study. Male and female rats were given a 4-hour IV infusion of eletriptan or sumatriptan to achieve steady state conditions. After 4 h, blood samples were collected terminally by heart puncture and tissues of interest were isolated including CNS regions: spinal cord, hypothalamus, striatum, cerebellum, brain stem, frontal cortex, and parietal cortex as well as whole brain, and PNS regions: trigeminal ganglion and sciatic nerve. Created with Biorender.com. B Total tissue-to-plasma concentration ratio (Kp). C The unbound tissue-to-plasma concentration ratio (Kp, uu). Columns represent mean ± SD (n = 4–6). The mean value of each column is annotated within each bar. The dotted line represents the line of unity. Values below unity indicate predominant active efflux across the respective barriers. In Fig. 3B and C, regions are sorted according to descending Kp/Kp,uu values for eletriptan. NB: in B and C a semilogarithmic scale is used for the visualization of data. Data are presented with a linear scale in Additional File 3