Effects of TRAM-34 on rat CYP Activity.

Abstract

<p>Recombinant enzyme CYP2C6 (A), CYP2C11 (B), CYP1A2r (C) and CYP2B1 (D), substrate and varying concentrations of TRAM-34 were incubated in the presence of 50 mM potassium phosphate buffer and regenerating system at 37°C according to the methods described. Percent control enzyme activity (ordinate) is plotted versus the log of inhibitor concentration (abscissa). All TRAM-34 and clotrimazole data points (A and B) represent the mean (±SEM) of 3 experiments performed in triplicates. Other clotrimazole data represent the mean of duplicates (C) or triplicates (D) from a single experiment. TRAM-34 IC₅₀ values were determined by non-linear regression and are shown in parentheses. Control enzyme activities were (mean ± SEM, n = 3 experiments each) 1.65±0.34 (<b>A</b>), 0.14±0.02 (<b>B</b>), 0.68±0.11 (<b>C</b>) and 6.13±0.7 (<b>D</b>) min^–1. In this and subsequent figures, error bars represent SEM of measurements, but, due to the small variability, are not always visible.</p