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. Author manuscript; available in PMC: 2021 Jul 23.
Published in final edited form as: J Med Chem. 2020 Jul 6;63(14):7569–7600. doi: 10.1021/acs.jmedchem.9b01733

Table 9.

Plasma Pharmacokinetics Comparison Between EU-1180–453 and CIQ

# dose (mg/kg)a Cmax (ng/mL) Cmax (μM) t1/2 (h) PPB, fubb [brain]: [plasma]c cLogP LLE (GluN2C/2D)
CIQ 20 2090 ± 20 2.16 ± 0.03 1.35 ± 0.12 <0.1 6.7 ± 2.2 5.6 −0.7/−1.1
EU-1180-453 10 695 ± 111 1.83 ± 0.29 1.07 ± 0.04 1.3 1.4 ± 0.5 4.5 1.2/1.2
a

Compounds were dosed i.p. in either 1:4:5 dimethylacetamide:PEG400:(5% dextrose in water) (CIQ, n = 3/group) or 1:1 PEG400:water (EU-1180–453, n = 3/group).

b

Rat plasma protein binding reported as percent unbound (fub ) at 1 μM.

c

Brain and plasma concentrations in ng/g and ng/mL, respectively, at Cmax.