TABLE 2

CLint, Vmax, and KM values for substrates and metabolites in suspensions and monolayer cultures of rat hepatocytes

Data are the mean ± S.D. of three determinations.

Metabolite
CLint
Vmax
KM or S50
Literature
Suspensiona
 Monolayer Culture
Suspensiona
 Monolayer Culture
Suspensiona
 Monolayer Culture
μl/min/106 cells nmol/min/106 cells μM
HTOL 1.6c 0.29 ± 0.05 0.35 ± 0.06* 0.39 ± 0.08 0.26 ± 0.09 1390 ± 490 720 ± 150
7-HCb 26d 38.6 ± 6.5 24.2 ± 8.2 0.0064 ± 0.0013 0.009 ± 0.001 0.18 ± 0.06 0.41 ± 0.12
4-OH PHEb 37c 12.0 ± 2.3 3.2 ± 0.9* 0.087 ± 0.036 0.013 ± 0.005* 7.6 ± 1.9 4.5 ± 2.4
4′-OH DZ 52.8 ± 18.3 17.2 ± 7.8* 0.20 ± 0.04 0.12 ± 0.05 4.4 ± 2.2 8.4 ± 4.3
NDZ 11.9 ± 2.3 2.3 ± 0.3* 0.40 ± 0.10 1.20 ± 0.99 36 ± 14 370 ± 282
TZ 25.5 ± 10.7 3.2 ± 1.3* 1.45 ± 0.53 0.29 ± 0.18 59 ± 22 148 ± 110
DZ total 82e 90.1 ± 22.5 22.7 ± 7.7*
DOR 54.3 ± 15.1 6.2 ± 1.6* 0.69 ± 0.06 0.36 ± 0.08* 9.2 ± 1.6§ 63 ± 28
MEM 43.2 ± 8.5 2.0 ± 0.4* 1.34 ± 0.20 0.57 ± 0.16* 21 ± 6§ 183 ± 100*§
DEX total 105f 97.6 ± 19.0 8.2 ± 1.3*
4-OH WAR 0.011 ± 0.0027 0.101 ± 0.049 0.0063 ± 0.0032 0.0036 ± 0.0011 542 ± 167 42 ± 18*
6-OH WAR 0.0068 ± 0.0028 0.026 ± 0.008* 0.0018 ± 0.0010 0.0015 ± 0.0004 261 ± 68 63 ± 31*
7-OH WAR 0.063 ± 0.021 0.135 ± 0.008* 0.0053 ± 0.0023 0.0039 ± 0.0021 83 ± 15 29 ± 14*
8-OH WAR 0.012 ± 0.0015 0.031 ± 0.010 0.018 ± 0.006 0.022 ± 0.003 1452 ± 424 742 ± 213*
10-OH WAR 0.004 ± 0.0016 0* 0.0008 ± 0.0002 0* 240 ± 159 0*
WAR total N.A. 0.097 ± 0.028 0.293 ± 0.048*
PROP
1800g
49 ± 8
8.9 ± 4.2*
N.D.
N.D.
N.D.
N.D.

  • N.A., data not available; N.D., parameters not determined.

    a Griffin and Houston (2004); b CLint values for both sites; Vmax and KM values for the high-affinity site only; c Ashforth et al. (1995); d Carlile et al. (1998); e Carlile (1994); fWitherow and Houston (1999); g Hallifax (1998).

  • ↵* Significant difference between fresh and cryopreserved suspensions (p < 0.05).

  • ↵§ Km values are given for all pathways except DOR and MEM (S50 values, sigmoidal kinetic).