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Table 1 Steady-State kinetic parameters and RAF weighted contributions for PQ metabolism

From: CYP450 phenotyping and accurate mass identification of metabolites of the 8-aminoquinoline, anti-malarial drug primaquine

 

Km(mM)

Vmaxa

Vmax/Kmb

RAFc

Contributiond

% Contributione

2D6

37 ± 3

35.2 ± 2.5

951.4

0.014

13.3

1.7

3A4

37 ± 2

3.6 ± 0.2

97.3

0.42

40.9

5.2

2 C19

52 ± 19

25.6 ± 9.5

492.3

0.24

118.2

17.0

MAO-A

17 ± 1

10.4 ± 0.5

615.4

0.97

596.9

76.1

  1. a Values in picomoles per minute per picomole of enzyme.
  2. b Values in nL/min/picomole of enzyme.
  3. c RAF = (rate for probe subs. with HLM)/(rate for probe subs. with isoenzyme).
  4. dContributioni = (rate of metabolism for unknown with isoenzyme).
  5. e% Contributioni = (Contributioni/(∑ Contribution values))*100.