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Table 6 UM-1 and UM-2 production after incubation with individual DHF stereoisomers.

From: The stereospecificity of flobufen metabolism in isolated guinea pig hepatocytes

 

peak area (AU × s × 104)

 

incubation time (h)

 

2

4

8

24

 

substrate (2R;4S)-DHF 50 μM

UM-1

-

-

-

18.0 ± 0.5

UM-2

8.7 ± 0.6

41.4 ± 3.7

72.1 ± 4.0

167.7 ± 8.0

 

substrate (2R;4S)-DHF 100 μM

UM-1

-

-

-

32.3 ± 0.2

UM-2

10.4 ± 0.1

48.2 ± 1.5

102.7 ± 6.1

228.6 ± 4.2

 

substrate (2S;4R)-DHF 50 μM

UM-1

-

-

-

31.1 ± 4.2

UM-2

10.0 ± 1.1

48.9 ± 5.0

95.4 ± 3.5

196.1 ± 11.7

 

substrate (2S;4R)-DHF 100 μM

UM-1

-

-

-

37.7 ± 3.3

UM-2

69.0 ± 0.5

43.0 ± 1.1

133.1 ± 7.3

237.5 ± 5.8

 

substrate (2S;4S)-DHF 50 μM

UM-1

-

-

-

18.9 ± 2.8

UM-2

71.7 ± 2.4

140.7 ± 5.5

171.3 ± 2.2

248.6 ± 15.8

 

substrate (2S;4S)-DHF 100 μM

UM-1

-

-

-

39.3 ± 2.2

UM-2

119.1 ± 7.5

228.1 ± 7.8

299.7 ± 18.7

401.5 ± 9.1

 

substrate (2R;4R)-DHF 50 μM

UM-1

-

-

-

21.9 ± 1.8

UM-2

11.2 ± 0.1

17.9 ± 0.1

69.7 ± 3.7

143.6 ± 8.3

 

substrate (2R;4R)-DHF 100 μM

UM-1

-

-

-

33.9 ± 3.3

UM-2

11.3 ± 8.1

28.3 ± 1.0

99.9 ± 4.4

193.4 ± 7.2

  1. UM-1 and UM-2 production in isolated guinea pigs hepatocytes after incubation with individual DHF stereoisomers (mean value ± S.D., n = 4).