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 |
Average n = 2, male Sprague–Dawley rats; dose = 1.0 mg/kg.
Calcium mobilization mGlu5 assay; values are an average of n ≥ 3 independent experiments.
t1/2 = Terminal phase plasma half-life; MRT = mean residence time; Clp = plasma clearance; VSS = volume of distribution at steady-state.
Vehicle = 10% EtOH, 70% PEG 400, 20% saline.
Vehicle = 10% EtOH, 60% PEG 400, 30% saline.
Vehicle = 10% EtOH, 50% PEG 400, 40% saline.