TABLE 5

Comparison of catalytic activity between two sets of microsomes at low selected substrate concentrations

Two-tailed unpaired t test used to compare groups 1 and 2.



Metabolite Formation Rate (pmol/min/mg)
Substrate
TST
ERM
MDZ
FLZ
CBZ
DXM
TFN
LDC
ITZ
Metabolite 6β-OH N-Desmethyl* 1′-OH* and 4 -OH 3-OH* + desmethyl 10,11-epoxide* 3-MM Alcohol* MEGX* ITZ-OH
Group 1
HL-102 951 43.3 129 171 37.9 25 201 112 7.49
HL-103 735 26.4 95 130 33.7 25 485 184 5.08
HL-109 712 26.5 134 143 49.1 37 167 62 4.74
HL-111 891 31.0 126 161 41.7 26 227 93 4.81
HL-115 705 26.5 115 88 13.8 22 246 35 4.17
HL-124 1830 86.4 264 198 72.7 41 247 141 9.58
HL-129 1860 72.4 289 267 71.4 38 295 121 8.55
HL-132 868 19.4 144 75 10.8 20 184 23 4.71
HL-168 1050 32.6 N.A. 205 29.8 24 229 122 6.16
HL-171 1110 43.5 N.A. 235 35.6 27 278 149 5.72
Mean ± S.D. 1071 ± 430 40.8 ± 21.9 162 ± 72 167 ± 61 39.7 ± 20.7 29 ± 7 256 ± 90 104 ± 51 6.10 ± 1.84
Group 2
HL-141 2050 72.7 421 507 94 80 382 286 8.47
HL-121 1320 65.7 260 313 35.6 41 344 54 8.27
HL-119 2020 90.0 300 370 92.3 61 649 146 10.98
HL-158 1810 69.3 274 334 67.2 15 286 123 8.06
HL-162 1190 49.3 167 271 32.2 33 232 257 6.98
HL-144 3910 161 651 552 120 101 480 221 14.67
HL-163 2460 89.6 368 571 115 80 280 183 9.66
HL-108 651 23.3 133 160 24.2 24 165 59 3.87
HL-125 1540 62.0 291 341 35.1 46 426 105 10.64
HL-147 1490 84.7 288 261 46.2 36 370 103 6.21
Mean ± S.D.
1844 ± 886
76.8 ± 35.8
315 ± 145
368 ± 135†††
66.2 ± 36.4
52 ± 28
361 ± 137
154 ± 81
8.78 ± 2.95
  • * Major metabolite formed in vivo; p < 0.05; †† p < 0.01; ††† p < 0.001.