Parameter | [3H]Morphine | [3H]M6G |
---|---|---|
Pharmacokinetics | ||
A 1(%ID/ml) | 1.66 ± 0.12 | 3.24 ± 0.43 |
A 2 (%ID/ml) | 0.228 ± 0.014 | 0.408 ± 0.084 |
K 1(min−1) | 0.868 ± 0.058 | 0.596 ± 0.001 |
K 2 (min−1) | 0.0189 ± 0.0013 | 0.0256 ± 0.0090 |
t 1/2 1 (min) | 0.806 ± 0.058 | 1.31 ± 0.28 |
t 1/2 2 (min) | 37 ± 3 | 36 ± 13 |
AUC0–60′ (% ID min/ml) | 10.1 ± 0.4 | 18.2 ± 0.9 |
AUC0–∞(% ID min/ml) | 14.0 ± 0.7 | 24.4 ± 4.7 |
Vc (ml/kg) | 220 ± 13 | 85 ± 10 |
Vss (ml/kg) | 1355 ± 73 | 453 ± 88 |
CL (ml/min/kg) | 29.5 ± 1.8 | 13.3 ± 2.5 |
MRT (min) | 46 ± 4 | 40 ± 16 |
Brain uptake | ||
Brain VD (μl/g) | 1005 ± 64 | 45 ± 19 |
PS (μl/min/g) | 8.03 ± 0.28 | 0.142 ± 0.026 |
% ID/g | 0.0810 ± 0.0005 | 0.00256 ± 0.00038 |
Lipid solubility | ||
P of 1-octanol/buffer | 0.207 ± 0.002 | 0.00111 ± 0.00007 |
Pharmacokinetic and organ uptake parameters were estimated from the plasma profile data during a 60-min period of observation in rats (mean ± SE, N = 3). The lipid solubility was determined in triplicate (mean ± SE) using the 1-octanol/buffer partition method.
t1/2, half-life;Vc , initial plasma volume;Vss , systemic volume of distribution;CL, plasma clearance; MRT, mean residence time;VD , volume of distribution.