Relative metabolite amounts of the fraction metabolized of sila-haloperidol
Liver microsomes incubated for 60 min and hepatocytes incubated for 120 min. Data estimated from integration of extracted ion chromatograms.
| Sila-haloperidol | |||||||
|---|---|---|---|---|---|---|---|
| Metabolite | m/z | tR (min) | RLM | HLM | Rat Heps | Dog Heps | Human Heps |
| Relative proportions of metabolites after incubation of sila-haloperidol for 60/120 min (%) | |||||||
| N-Dealk | 228 | 1.22 | 21 | 11 | 44 | 5 | 12 |
| Ring-opened1+OH | 380 | 1.28 | 2 | 2 | 0 | 0 | 0 |
| +OH+Gluc | 584 | 1.52 | N.D. | N.D. | 39 | 0 | 0 |
| Ring-opened1 | 364 | 1.74 | 4 | 63 | 0 | 10 | 25 |
| +OH+Sulfate | 488 | 1.82 | N.D. | N.D. | 3 | 0 | 0 |
| OH | 408 | 1.90 | 71 | 3 | 5 | 0 | 0 |
| Ring-opened2 | 382 | 1.94 | 1 | 20 | 0 | 2 | 7 |
| Red | 394 | 2.01 | 1 | 1 | 9 | 84 | 56 |
| Fraction of parent drug remaining after incubation (%) | |||||||
| Sila-haloperidol | 392 | 2.18 | 83 | 65 | 80 | 61 | 94 |
Heps, hepatocytes; N.D., not determined (no addition of UDPGA in this experiment).