TABLE 1

Pharmacokinetic properties of NS1738

Rats (n = 3) were dosed with 10 mg/kg i.p. NS1738 at time 0, and plasma samples were collected at 0, 15, 30, 60, and 120 min and analyzed by mass spectrometry for their NS1738 content. Assuming the pharmacokinetics of NS1738 to be approximated by one-compartment distribution and first-order elimination, estimates for Tmax, t1/2, Cmax, and AUC were calculated, as displayed in the table. The brain/plasma distribution ratio was estimated by measuring plasma and brain concentrations at the same time points as listed above, following administration of 10 mg/kg i.p. NS1738 (n = 3). The brain-plasma ratio was subsequently calculated as AUCbrain/AUCplasma.


Species

Dose

Tmax

t1/2

Cmax

AUC

Brain-Plasma Ratio

Microsomal Stability (% Left at 1 h)
mg/kg i.p. min ng/ml ng ยท min/ml
Rat
10
30
42
172
13,381
0.50
mouse:41 rat:25