TABLE 5

Pharmacokinetic parameters of CP-615,003 (40 mg/kg p.o.) and CP-900,725 (two doses of 10 mg/kg s.c.) in rat serum and brain ECF by intracerebral microdialysis

Compound
Pharmacokinetic Parameter
Serum
Brain ECF
CP-615,003 AUCteq-inf (h · ng/ml)a 19037 ± 10651 25.1 ± 10.3
t1/2 (h) 2.56 ± 0.17 2.89 ± 0.37
K p, ECF 0.00143 ± 0.00035**
CP-900,725 AUCteq-inf (h · ng/ml)a 5348 ± 182 77.6 ± 30.8
t1/2 (h) 3.36 ± 2.01 1.26 ± 0.35
K p, ECF
0.0145 ± 0.0060*

  • ↵ a Area under the plasma or ECF concentration-time profile from the time of microdialysis probe reaching equilibrium (teq) until infinity (tinf).

  • ↵* p < 0.05, when compared against the serum free fraction.

  • ↵** p < 0.01, when compared against the serum free fraction.