Table 3.
Specific activity of hCE1, hCE2, hCE3, and FAAH towards 2-methyl-6-methoxy-3-pyridinyl amides with varying acyl chains. Substrate activities ([S] = 50 µM) were measured at 37°C in phosphate buffer (100 mM, pH = 8, 0.1 mg/mL BSA) containing 1% DMSO. Values represent the average of triplicates for a single experiment.
| ||||||
|---|---|---|---|---|---|---|
|
| ||||||
| No. | R | x | hCE1a | hCE2b | hCE3c | Ratio hCE1/hCE2 |
|
| ||||||
| Specific activity (pmol.min−1.µg−1) | ||||||
| 2 |
|
0 | 1.1 | <1 | <1 | n/a |
| 3 | 2 | 6.8 | 14 | <1 | 0.5 | |
| 4 | 4 | 53 | 36 | 2.3 | 1.5 | |
| 5 | 5 | 180 | 28 | 3.9 | 6.4 | |
| 1a | 6 | 440 | 33 | 6.0 | 13 | |
| 6 | 7 | 390 | 37 | 8.5 | 11 | |
| 7 | 8 | 130 | 30 | 10 | 4.3 | |
| 8 | 10 | 19 | 29 | 9.8 | 0.7 | |
| 9 | 12 | 2.6 | 25 | 7.8 | 0.1 | |
| 10 |
|
0 | <1 | <1 | <1 | n/a |
| 11 | 1 | <1 | <1 | <1 | n/a | |
| 12 |
|
0 | 2.3 | 3.2 | <1 | 0.7 |
| 13 | 1 | 2.9 | <1 | <1 | n/a | |
| 14 | 2 | 6.3 | 7.1 | <1 | 0.9 | |
| 15 | 3 | 190 | 4.9 | <1 | 38.8 | |
| 16 | 4 | 93 | 18 | <1 | 5.2 | |
| 17 | 5 | 52 | 5.4 | 1.6 | 9.6 | |
| 18 | 7 | 82 | 30 | 10 | 2.7 | |
| 19 (4-MOMMP) |
|
0 | 450 | 13 | <1 | 35 |
| 20 |
|
0 | 510 | 18 | 4 | 28 |
Values were calculated based on estimated of 25%.
Values were calculated based on estimated of 4%.
Values were calculated based on estimated of 3%.