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. 2011 Jul 29;2(10):752–757. doi: 10.1021/ml2001399

Table 3. Pharmacokinetic Profile of Carbamoylnicotinamide 8a.

  1 mg/kg iv
     
PPBb (%) rat CLc (L/h/kg) Vdssc (L/kg) T1/2c (h) AUC0→48 hc (ng h/mL) AUC0→48 hd (ng h/mL) 3 mg/kg po Fe (%) AUC0→48 hf (ng h/mL) 100 mg/kg po
95 0.25 6.3 19 3400 13000 140 350000
a

In vivo experiments were conducted using male Sprague–Dawley rats (N = 3/group).

b

Percent rat plasma protein binding (PPB) of 8 measured in vitro following separation by ultracentrifugation.

c

Clearance (CL), volume of distribution (Vdss), half-life (T1/2), and area under the plasma concentration–time curve (AUC0→48 h) determined following a single intravenous dose (1 mg/kg; vehicle = DMSO).

d

AUC0→48 h determined following a single oral dose (3 mg/kg; vehicle = 20% HPBCD, 1% HPMC, and 1% pluronic F68, pH 2.1, with MSA).

e

Percent bioavailability (F) calculated using AUC0→∞ values determined from the 1 (iv) and 3 mg/kg (po) doses.

f

AUC0→48 h determined following a single oral dose (100 mg/kg; vehicle = 20% HPBCD, 1% HPMC, and 1% pluronic F68, pH 2.1, with MSA).