Table 2.
Affinity of ligands for CB1R and CB2R.
| Ligands | Ki for CB1R (nM) | Ki for CB2R (nM) | References |
|---|---|---|---|
| Endogenous ligands | |||
| 2-arachidonolyglycerol | 58.3-472 | 145-1400 | (43, 54, 91) |
| Anandamide | 61-543 | 279-1940 | (43, 54, 91) |
| Exogenous ligands | |||
| MRI-1867# | 1.2-8.0 | >1000 | (105) |
| WIN55,212-2 | 1.89-123 | 0.28-16.2 | (106, 107) |
| SR141716A (rimonabant) | 1.98-12.3 | 702-13200 | (108) |
| JD5037 | 2 | >1000 | (109, 110) |
| AM6545 | 3.3 | 624 | (38, 111) |
| Δ9-THC | 5.05-80.3 | 3.13-75.3 | (107) |
| AM251 | 7.49 | 2290 | (112, 113) |
| (S)-SLV 319 (ibipinabant) | 7.8 | 7.9 | (114) |
| AM281 | 12 | 4200 | (115) |
| (R)-Methanandamide | 17.9-28.3 | 815-868 | (116) |
| SR144528 | 400 | 0.6 | (117) |
| AM1241 | 580 | 7 | (118) |
| JWH-133 | 677 | 3.4 | (119) |
| AM630 | 5152 | 31.2 | (120) |
CB1R, cannabinoid receptor type 1; CB2R, cannabinoid receptor type 2; Ki, inhibition constant; THC, tetrahydrocannabinol.
#MRI-1867 is a dual CB1R/inducible NOS antagonist.