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Table 1 Biotransformation of rac-F, R-F and S-F in isolated guinea pig hepatocytes.

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

Substrate

Incubation time [h]

Apparent actual clearance [h-1 × 10-3]

  

M-17203

(2R;4S)-DHF

(2S;4R)-DHF

(2S;4S)-DHF

(2R;4R)-DHF

 

2

1.8 ± 0.7

111.2 ± 8.6

10.8 ± 0.1

57.5 ± 5.0

2.3 ± 0.0

 

4

1.4 ± 0.2

67.7 ± 0.5

7.1 ± 0.4

42.4 ± 0.6

0.8 ± 0.1

rac -F

      
 

8

1.6 ± 0.1

22.8 ± 1.3

1.6 ± 0.2

12.8 ± 1.0

0.1 ± 0.0

 

24

3.8 ± 0.8

4.2 ± 0.2

0.3 ± 0.0

3.6 ± 0.1

-

 

2

1.6 ± 0.5

147.1 ± 11.8

1.6 ± 0.4

38.0 ± 3.8

6.3 ± 0.5

 

4

1.2 ± 0.1

91.1 ± 2.7

3.4 ± 0.1

33.6 ± 1.4

2.0 ± 0.1

R-F

      
 

8

1.4 ± 0.1

32.3 ± 0.8

1.0 ± 0.8

12.9 ± 0.1

0.2 ± 0.0

 

24

2.9 ± 0.0

7.6 ± 1.4

0.2 ± 0.0

4.5 ± 0.5

-

 

2

2.9 ± 0.2

58.1 ± 3.2

13.3 ± 0.7

56.9 ± 2.6

-

 

4

2.4 ± 0.3

47.3 ± 1.5

10.2 ± 1.0

44.6 ± 2.1

0.5 ± 0.3

S-F

      
 

8

2.0 ± 0.1

20.0 ± 0.4

3.7 ± 0.1

15.8 ± 0.2

0.1 ± 0.0

 

24

3.0 ± 0.2

4.3 ± 0.5

0.6 ± 0.0

4.9 ± 0.4

0.4 ± 0.1

  1. Apparent actual clearance (Claa) of F metabolites in the isolated hepatocytes after incubation with 100 μM rac-F, R-F and S-F as substrates. Claa is expressed as the ratio of actual velocity (mol/l/h) and substrate concentration (mol/l), (mean value ± S.D., n = 4).
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BMC Pharmacology

ISSN: 1471-2210