In vitro metabolism of the α1-adrenoceptor antagonists in series 2
Compound | Human Liver Microsomes | Dog Liver Microsomes | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Half-life | fu(inc) | CLint,un | Half-life | fu(inc) | CLint,un | |||||
| min | ml/min/kg | min | ml/min/kg | |||||||
| UK-294,15 | 6 | 0.331 | 154 | 30 | 0.602 | 100 | ||||
| 2 | 9 | 0.414 | 82 | 25 | 0.59 | 122 | ||||
| 3 | 5 | 0.637 | 96 | 14 | 0.791 | 162 | ||||
| 4 | 9 | 1 | 34 | 46 | 0.939 | 41 | ||||
| 5 | 19 | 0.745 | 22 | 80 | 0.962 | 23 | ||||
| 6 | 31 | 0.823 | 12 | 36 | 1 | 50 | ||||
| UK-338,003 | 41 | 0.564 | 13 | 36 | 0.602 | 83 | ||||
CLint,un' unbound intrinsic clearance.