Table 1. Inhibition of hsEH and Microsomal Stability Values of the New Benzohomoadamantane-Based sEHI.
| Cpd | hsEHaIC50 (nM) | microsomal stabilityb (h/m/r) |
|---|---|---|
| 9 | 138 | NDc |
| 11 | >10,000 | ND |
| 7 | 7.7 | 79/77/81 |
| 13 | 1.0 | 7/0.2/ND |
| 14 | 20 | 77/23/33 |
| 1, AR9281 | 8.0 | 72/100/87 |
| 16 | 3.1 | 1/0.5/ND |
| 17 | 941 | ND |
| 18 | >10,000 | ND |
| 4, t-AUCB | 0.5 | 94/92/46 |
| 20 | 0.9 | 70/10/2 |
| 21 | 28 | 90/83/ND |
a
Reported IC50 values are the average of three replicates. The fluorescent assay as performed here has a standard error between 10 and 20% suggesting that differences of twofold or greater are significant. Because of the limitations of the assay, it is difficult to distinguish among potencies <0.5 nM.16
b
Percentage of the remaining compound after 60 min of incubation with human, mice, and rat microsomes obtained from Tebu–Xenotech in the presence of NADP at 37 °C.
c
ND: not determined.