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. 2017 May 22;60(12):5072–5085. doi: 10.1021/acs.jmedchem.7b00410

Table 4. Preliminary Rat PK Results Using Intravenous (IV) Dosinga.

no. mGlu5 IC50 (nM)b t1/2 (min)c MRT (min)c Clp (mL/min/kg)c VSS (L/kg)c
21d 20 105 39 34.2 1.6
22e 9.1 268 120 32.5 4.5
23f 9.3 404 80 43.7 6.6
26d 3.6 82 157 96 11
27d 11 390 93 19.3 1.8
28d 3.1 281 208 9.2 1.9
33f 33 229 191 6.2 1.2
a

Average n = 2, male Sprague–Dawley rats; dose = 1.0 mg/kg.

b

Calcium mobilization mGlu5 assay; values are an average of n ≥ 3 independent experiments.

c

t1/2 = Terminal phase plasma half-life; MRT = mean residence time; Clp = plasma clearance; VSS = volume of distribution at steady-state.

d

Vehicle = 10% EtOH, 70% PEG 400, 20% saline.

e

Vehicle = 10% EtOH, 60% PEG 400, 30% saline.

f

Vehicle = 10% EtOH, 50% PEG 400, 40% saline.