Species | System | Reference | Km | Vmax1-a | V/K1-b | In vitro t1/2 | CLint′ | Well-stirred CLb |
---|---|---|---|---|---|---|---|---|
μM | ml/min/mg | min | ml/min/kg | |||||
Human | FMO3 | Lang and Rettie, 2000 | 80 ± 8 | 36 ± 2 | 0.04 | 34.0 | 12.6 | |
HLM | Stormer et al., 2000 | 64 ± 17 | 6.9 ± 3.6 | 0.11 | 101.9 | 16.7 | ||
Rat | RLM | Kawaji et al., 1993 | 15 ± 1 | 37 ± 3 | 2.47 | 4446.0 | 68.9 | |
Human | hepatocytes | 145 | 51.7 | 14.4 | ||||
HLM+NADPH1-c | 8.9 | 38.4 | 13.2 | |||||
HLM-NADPH | 15.1 | 22.6 | 10.6 | |||||
Rat | hepatocytes | 2.3 | 3254.1 | 68.5 |
Benzydamine in vivo CL = 2.4 ml/min/kg (Chasseud and Catanese, 1985; Schoenwald et al., 1987) assuming a 70 kg human.
RLM, rat liver microsomes; HLM, human liver microsomes.
↵1-a Vmax in nmol/min/mg, except FMO3 in nmol/min/nmol.
↵1-b FMO3 V/K, in ml/min/nmol, was converted to ml/min/mg assuming 80 pmol/mg human liver microsomes (Haining et al., 1997).
↵1-c HLM were prewarmed with or without NADPH present, and reaction was initiated with either NADPH or substrate.