Table 2. Pharmacokinetic Parameters of Oxadiazolesa.
cmpd | dose (mg/kg) | AUC0–∞ (μg·min/mL) | Cmax (μg/mL) | Tmax (h) | CL (mL/min/kg) | Vd (mL/kg) | t1/2 | F (%) |
---|---|---|---|---|---|---|---|---|
2 | 50 iv | 1380 | 36.2 | 860 | t1/2α = 2.4 min | |||
t1/2β = 4.4 h | ||||||||
3 | 50 iv | 2650 | 18.9 | 370 | t1/2α = 3.5 min | |||
t1/2β = 22 h | ||||||||
50 po | 2620 | 2.5 | 2 | t1/2abs = 3.3 h | ∼100 | |||
t1/2dist = 6.0 h | ||||||||
t1/2elim = 40 h | ||||||||
4 | 50 iv | 9200 | 5.4 | 720 | t1/2α = 6.7 min | |||
t1/2β = 20 h | ||||||||
50 po | 9220 | 10.0 | 2 | t1/2abs = 2.4 h | 100 | |||
t1/2dist = 13 h | ||||||||
t1/2elim = 36 h |
n = 3 mice per time point per route of administration; 10–12 time points. AUC0–∞, area under the plasma concentration–time curve from 0 to infinity; Cmax, maximum concentration observed in plasma; Tmax, time at which maximum plasma concentration is observed; CL, plasma clearance; Vd, volume of distribution; t1/2α, initial half-life; t1/2β, terminal half-life; t1/2abs, absorption half-life; t1/2dist, distribution half-life; t1/2elim, elimination half-life; F, oral bioavailability.