Table 1.
Summary of the pharmacological effects exerted by MH, 27a, 32, and 34a
| IC 50 or K i values (mean value ± SD, μM) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| h COX-2 | RAW264.7 Intact cells | CHO membranes | CHO cells | Pig brain homog. | BV-2 homog. | U937 cells | ||||||
| AA | 2-AG | AA | 2-AG | h CB 1 | h CB 2 | h CB2 [ 35 S] GTPγS | h CB2 cAMP | FAAH | MAGL | ABHDs | AEA uptake | |
| MH | 0.58 ± 0.08 | **0.15 ± 0.09 | 1.56 ± 0.12 | **0.28 ± 0.09 | 2.4 ± 0.6 | 0.19 ± 0.12 | 0.20 ± 0.10 | 0.67 ± 0.07 | >10 | >10 | >10 | 6.5 ± 1.2 |
| 27a | 1.21 ± 0.08 | **0.42 ± 0.09 | 0.98 ± 0.08 | **0.28 ± 0.11 | 0.79 ± 0.10 | 0.11 ± 0.09 | 0.18 ± 0.09 | 0.71 ± 0.09 | >10 | >10 | >10 | >10 |
| 32 | 10.2 ± 0.12 | **0.63 ± 0.05 | 2.8 ± 0.22 | **0.21 ± 0.14 | >10 | >10 | n.d. | n.d. | >10 | >10 | >10 | 6.3 ± 1.6 |
| 34a | 4.31 ± 0.10 | *1.29 ± 0.07 | >30 | **1.57 ± 0.13 | 1.12 ± 0.15 | 0.35 ± 0.11 | 1.82 ± 0.14 | 1.52 ± 0.13 | >10 | >10 | >10 | >10 |
| DuP-697 | 0.061 ± 0.005 | 0.07 ± 0.01 | 0.004 ± 0.004 | 0.005 ± 0.006 | n.d. | n.d. | n.d. | n.d. | n.d. | n.d. | n.d. | n.d. |
The data are expressed as mean ± SD of at least three independent experiments each performed in triplicates. Binding affinity to CB1 and CB2 receptors is expressed as K i value while modulation of CB2 receptor activation (cAMP and [35S] GTPγS) and inhibition of enzyme activity and AEA uptake are expressed as IC50 value. *P < 0.05; **P < 0.01 PGE2-GE vs. PGE2. n.d.: not determined P < 0.05; **P < 0.01 PGE2-GE vs. PGE2. Items in bold are compound abbreviations.