Inhibition kinetics of CYP3A activity by mitragynine in HIM CSV JSON

In Vitro Enzyme Inhibition Experiment

Inhibition kinetics of CYP3A activity by mitragynine in HIM

Inhibition was detected.  Cutoff used —

N/A

midazolam 708298

mitragynine

1'-hydroxymidazolam

  • CYP3A

Cell fraction Pooled human intestinal microsomes -7999663

Results

The KIand kinactvalues for mitragynine towards CYP3A activity in HIM were 4.5  ± 1.1 µM and 0.072  ± 0.006 min-1,  6.0  ± 0.5 µM and 0.074  ± 0.002 min-1, and  7.3  ± 2.5 µM and 0.17  ± 0.02 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

1610314

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