Table 1

Pharmacokinetic parameter estimates for CPA analogs obtained after intravenous infusion for 15 min in conscious rats

k10k12k21VC
min−1 ml
2′dCPA0.18  ± 0.000.098  ± 0.0090.018  ± 0.006184  ± 19
(31%)(144%)(18%)(13%)
3′dCPA0.39  ± 0.130.58  ± 0.260.14  ± 0.01138  ± 12
(21%)(0%)(72%)(0%)
5′dCPA0.39  ± 0.060.28  ± 0.050.071  ± 0.01264  ± 9
(10%)(0%)(23%)(0%)
8MCPA0.14  ± 0.010.12  ± 0.040.064  ± 0.009108  ± 15
(33%)(12%)(22%)(0%)
8ECPA0.12  ± 0.010.030  ± 0.0080.039  ± 0.006119  ± 15
(17%)(50%)(19%)(18%)
8BCPA0.10  ± 0.070.045  ± 0.0080.027  ± 0.004129  ± 10
(7%)(13%)(0%)(1%)

Parameter estimates (mean ± S.E.; n = 6–8) ofk10 (rate constant of elimination),k12 (rate constant for transfer from central to peripheral compartment), k21 (rate constant for transfer from peripheral to central compartment), andVC (volume of central compartment) were obtained by fitting the time-concentration data to a two-compartment model with NONMEM as described in the text. Estimates of interindividual variability are shown as CV in parentheses.