Table 4.
Data non-supporting the presence of novel endothelial cannabinoid receptor
| Read-out assay | Species/vascular bed | Agonist | pEC50 | Reference |
|---|---|---|---|---|
| PTX-insensitive relaxation to CB | RSMA | Abn-CBD | 6.2 μM | Ho and Hiley, 2003a; |
| RMA | Abn-CBD | 2 μM | Milman et al., 2006 | |
| RMA | ARA-S | 0.55 μM | Milman et al., 2006 | |
| RSMA | VSN16 | 88 nM | Hoi et al., 2007 | |
| RSMA | THC | 5.37 μM | O'Sullivan et al., 2005a | |
| PTX-sensitive EDR to A23187 | RSMA | A23187 | 6.46 μM | White and Hiley, 1997 |
| pEC50 | ||||
| Lack or minor EDR to CB | RabA | Abn-CBD | 0.01–0.3 μM tested | Su and Vo, 2007 |
| RCA | AEA | 6.8 μM | White et al., 2001 | |
| RSMA | AEA | 6.3 μM | White and Hiley, 1997 | |
| RMA | AEA | 5.0 μM | O'Sullivan et al., 2004 | |
| RMA | AEA | 0.3 μM tested | Randall et al., 1996 | |
| RA | AEA | 5.9 μM | O'Sullivan et al., 2005b | |
| RMA | AEA | 6.2 μM | Harris et al., 2002 | |
| RSMA | AEA | 6.7 μM | Ho and Hiley, 2003b | |
| RSMA | THC | 5.37 μM | O'Sullivan et al., 2005a | |
| RMA | THC | 1–10 μM tested | O'Sullivan et al., 2005a | |
| Rimonabant, μM | ||||
| Rimonabant inhibits vasodilatation to non-CB agonists/Ca2+ ionophores | RMA | Ionomycine | 5 μM | Wagner et al., 1999 |
| RCA | Bradykinin | 1 μM | Randall et al., 1997 | |
| RMA | Bradykinin | 1 μM | Randall et al., 1996 | |
| RMA | A23187 | 1 μM | Randall et al., 1996 | |
| RMA | Carbachol | 1 μM | Randall et al., 1996 | |
| RSMA | Carbachol | 1 μM | White and Hiley, 1997 | |
| O-1918, μM | ||||
| No effect of O-1918 on EDR O-1918 inhibits endothelium-independent relaxation | RA | ARA-S | 10 μM | Milman et al., 2006 |
| MA | ARA-S | 10 μM | Milman et al., 2006 | |
| RabPA | Abn-CBD | 0.1–1 μM | Su and Vo, 2007 | |
| RSMA | NAGly | 3 μM | Parmar and Ho, 2010 | |
| RSMA | SNP | 3 μM | Parmar and Ho, 2010 | |
| GPCR-independent targets for O-1918 | Targets | Effect | Concentration tested | |
| NCX | Inhibition | 10 μM | Bondarenko et al., 2013 | |
| BKCa | Inhibition | pIC50 = 6.6 μM | Godlewski et al., 2009 |
Abn-CBD, abnormal cannabidiol; AEA, anandamide; ARA-S, N-arachidonyl serine; BKCa, high-conductance Ca2+-dependent K+ channels; CB, cannabinoid; EDR, endothelium-dependent relaxation; NCX, Na+-Ca2+ exchanger; PTX, pertussis toxin; RA, rat aorta; RabA, rabbit aorta; RabPA, rabbit pulmonary artery; RCA, rat coronary artery; RMA, rat mesenteric artery; RSMA, rat small mesenteric artery; SNP, sodium nitroprussid; THC, Δ9-tetrahydrocannabinol; VSN16, 3-(5-dimethylcarbamoyl-pent-1-enyl)-N-(2-hydroxy-1-methyl-ethyl)benzamide.