Constants and data used as initial estimates for fitting of morphine and M3G data from the single-pass perfused rat liver preparation of M
Description | Assigned or Observed Value |
|---|---|
| Volume | |
| Liver sinusoid VE (ml/g liver) | 0.22a |
| Liver tissue Vt (ml/g liver) | 0.63a |
| Fractions unbound for morphine and M3G{mi} | |
| Unbound fraction of M in plasma (4% BSA), fu | 0.89b |
| Unbound fraction of M in blood, fu,b or Cp,u/Cblood | 0.654b |
| Unbound fraction of M in tissue, ft | 0.654b |
| Unbound fraction of M3G in plasma, fu{mi} | 1 |
| Unbound fraction of M3G in tissue, ft{mi} | 1 |
| Flow | |
| Hepatic blood flow rate: Q (ml min–1 g–1 liver) | 0.82 |
| Morphine: Michaelis-Menten constants and intrinsic clearances | |
| Sinusoidal influx: CLin = influx clearance (ml min–1 g–1) | 1.5 |
| Sinusoidal efflux: CLef = efflux clearance (ml min–1 g–1) | 1.5 |
| Biliary excretion from regression | |
| Vmax,ex (nmol min–1 g–1) | 6.76c |
| Km,ex (μM) | 23.4c |
| CLint,sec (ml min–1 g–1) | 0.289 |
| Glucuronidation from regression | |
| Vmax,met (nmol min–1 g–1) | 50.4c |
| Km,met (μM) | 74.5c |
| CLint,met (ml min–1 g–1) | 0.677 |
| M3G: first-order rate constants | |
| Sinusoidal influx: km1 (min–1) | 0.306d |
| Sinusoidal efflux: km2 (min–1) | 0.120d |
| Canalicular efflux: km3 (min–1) | 0.246d |