Comparison of in vitro binding affinity of SCH58235 and SCH60663 with in vivo potency of SCH58235 among several species
The Ki values of SCH58235 and its glucuronide metabolite SCH60663 are shown. Available in vivo potency data from previous studies (van Heek et al., 1997, 2001a,b,c; Davis, 2001; Davis et al., 2001b) is also displayed for comparison.
Species | Ki | SCH 58235 ED50 | ||
|---|---|---|---|---|
| SCH 58235 | SCH 60663 | |||
| nM | nM | μg/kg | ||
| Human | 1590 ± 200 | 660 ± 190 | N.D. | |
| Monkey | 900 ± 200 | 92 ± 10 | 0.5 | |
| Hamster | 1530 ± 350 | 370 ± 80 | 40 | |
| Canine | 770 ± 160 | 192 ± 40 | 7 | |
| Rat | 970 ± 280 | 352 ± 110 | 30 | |
| Rabbit | 2350 ± 210 | 830 ± 160 | N.D. | |
| Mouse | 9000 ± 1600 | 5400 ± 970 | 700 | |
N.D., not determined.