Human liver (A) and kidney (B) microsomes and UGT1A9 (C) bacculosomes were incubated with UDPGA (1 mM), in the presence of increasing concentrations of propofol (P, 1, 10, 50 and 100 μM) and pure (S)bicalutamide (5, 15, 25, 50, 150 and 500μM) for 2 hours at 37°C. Propofol-G formation was analyzed by LC-MS/MS, and Dixon plots analyses were performed to calculate the apparent Ki values. Data represent the mean ± S.D. of two independent experiments performed in triplicate.
G: glucuronide; P: propofol, V: propofol-G formation expressed as the ratio of the area under the curve (AUC) for propofol-G versus AUC of 4-methylumbelliferone-G/min/mg of proteins); Ki: constant of inhibition.