Activities of P450 isoforms and hCE1 in individual human liver microsomes
The P450 activities were determined by measuring the following activities: CYP1A2, phenacetin deethylation; CYP2B6, 7-benzyloxyresorufin debenzylation; CYP2C9, tolbutamide methylhydroxylation; CYP2C19, S-mephenytoin 4′-hydroxylation; CYP2D6, debrisoquine 4-hydroxylation; CYP2E1, chlorzoxazone 6-hydroxylation; CYP3A4, diazepam 3-hydroxylation. The hCE1 activity was determined by analyzing hydrolysis of temocapril. n = 20.
| Activity | ||||||||
|---|---|---|---|---|---|---|---|---|
| CYP1A2 | CYP2B6 | CYP2C9 | CYP2C19 | CYP2D6 | CYP2E1 | CYP3A4 | hCE1 | |
| pmol/mg/min | ||||||||
| HLM-009-1 | 1.02 | 0.37 | 4.00 | 9.00 | 35.00 | 23.0 | 52.0 | 7804.0 |
| HLM-012-1 | 10.14 | 0.52 | 5.00 | 3.00 | 16.00 | 48.0 | 120.0 | 15,830.0 |
| HLM-014-3 | 85.27 | 5.95 | 190.00 | 40.00 | 73.00 | 31.0 | 2100.0 | 40,300.5 |
| HLM-056-1 | 34.00 | 0.27 | 40.47 | 4.39 | 0.00 | 2570.0 | 277.2 | 19,595.0 |
| HLM-057-1 | 8.97 | 0.36 | 11.55 | 0.00 | 40.28 | 555.8 | 1159.0 | 12,769.0 |
| HLM-059-1 | 98.02 | 1.45 | 89.47 | 50.70 | 21.36 | 1258.0 | 1491.0 | 32,470.0 |
| HLM-061-1 | 182.92 | 2.61 | 74.45 | 8.26 | 14.79 | 1537.7 | 4010.6 | 41,414.5 |
| HLM-062-1 | 7.42 | 0.70 | 13.54 | 0.93 | 28.72 | 773.9 | 1544.9 | 11,473.5 |
| HLM-087-1 | 5.32 | 0.48 | 18.00 | 0.00 | 31.01 | 2095.2 | 1469.7 | 9886.0 |
| HLM-089-1 | 7.23 | 1.13 | 150.75 | 9.47 | 67.28 | 2404.0 | 3010.4 | 21,509.0 |
| HLM-090-1 | 15.91 | 0.39 | 76.26 | 1.52 | 2.13 | 2286.1 | 1672.5 | 17,608.5 |
| HLM-101-1 | 27.45 | 0.40 | 57.36 | 40.56 | 61.37 | 2241.9 | 2255.7 | 14,409.5 |
| HLM-104-1 | 25.79 | 1.75 | 52.13 | 2.17 | 2.62 | 4130.5 | 3823.6 | 17,833.0 |
| HLM-105-1 | 48.71 | 1.30 | 90.88 | 3.19 | 31.49 | 1879.7 | 3170.2 | 19,704.0 |
| HLM-116-1 | 35.25 | 1.79 | 65.79 | 8.23 | 24.30 | 2681.5 | 11727.0 | 15,076.5 |
| HLM-138-1 | 51.43 | 3.62 | 57.22 | 3.58 | 16.91 | 1606.0 | 866.5 | 24,086.0 |
| HLM-152-1 | 33.63 | 1.41 | 28.85 | 2.28 | 5.40 | 1036.0 | 278.1 | 20,349.0 |
| HLM-170-1 | 50.62 | 3.81 | 22.20 | 4.07 | 5.87 | 550.6 | 786.1 | 19,032.5 |
| HLM-188-1 | 42.23 | 11.13 | 0.64 | 8.07 | 56.38 | 1907.0 | 1238.0 | 23,808.0 |
| HLM-225-1 | 9.41 | 1.25 | 46.90 | 2.92 | 11.90 | 832.0 | 643.0 | 21,034.5 |
| Mean | 39.0 | 2.0 | 54.8 | 10.1 | 27.3 | 1522.4 | 2084.8 | 20,299.7 |
| S.D. | 42.8 | 2.6 | 49.2 | 14.9 | 22.4 | 1066.2 | 2557.8 | 8943.0 |
| CV (%) | 110 | 130 | 90 | 148 | 82 | 70 | 123 | 44 |