stage.napdi.org

Inhibition kinetics of CYP3A activity by mitragynine in HLM CSV JSON

In Vitro Enzyme Inhibition Experiment

Inhibition kinetics of CYP3A activity by mitragynine in HLM

Inhibition was detected.  Cutoff used —

N/A

midazolam 708298

mitragynine

1'-hydroxymidazolam

  • CYP3A

Cell fraction Pooled human liver microsomes -7999662

Results

The KIand kinactvalues for mitragynine towards CYP3A activity in HLM were 4.1  ± 0.7 µM and 0.051  ± 0.002 min-1,  4.0  ± 0.5 µM and 0.057  ± 0.002 min-1, and  5.9  ± 0.9 µM and 0.17  ± 0.01 min-1, respectively, for three individual experiments.
[KIand kinact(Mean ± SEM) values were determined using nonlinear least-squares regression.]

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Methanol (0.8 % v/v) served as solvent control. 6',7'-Dihydroxybergamottin (1 and 2 µM) served as a positive control inhibitor of CYP3A activity.

NA

0.05 mg/mL

Commercially available

1010191

NADPH

Available

Available

20 µM

1100 µL

0, 2, 5, 10, and 20 min

NADPH with precipitant

200 µL

5 min

No dilution

0.56 - 30 µM