Ki values of certain ligands for the in vitro displacement of [3H]CP55940, [3H]R-(+)-WIN55212, or [3H]HU-243 from CB1- and CB2-specific binding sites
| Ligand | CB1KiValue | CB2Ki Value | Reference |
|---|---|---|---|
| nM | |||
| CB1-selective ligands in order of decreasing CB1/CB2 selectivity | |||
| ACEA | 1.42-a 2-b | >2,0002-a 2-b | Hillard et al., 1999 |
| O-1812 | 3.42-b | 3,8702-b | Di Marzo et al., 2001a |
| SR141716A | 11.8 | 13,200 | Felder et al., 1998 |
| 11.8 | 973 | Felder et al., 1995 | |
| 12.3 | 702 | Showalter et al., 1996 | |
| 5.6 | >1,000 | Rinaldi-Carmona et al., 1994 | |
| 1.982-b | >1,0002-b | Rinaldi-Carmona et al., 1994 | |
| AM281 | 122-b | 4,2002-c | Lan et al., 1999a |
| ACPA | 2.22-a 2-b | 7152-a 2-b | Hillard et al., 1999 |
| 2-Arachidonylglyceryl ether | 21.22-b | >3,000 | Hanus et al., 2001 |
| LY320135 | 141 | 14,900 | Felder et al., 1998 |
| R-(+)-methanandamide | 17.92-a 2-b | 8682-a 2-c | Lin et al., 1998 |
| 202-a 2-b | 8152-c | Khanolkar et al., 1996 | |
| Ligands without any marked CB1/CB2 selectivity | |||
| Anandamide | 612-a 2-b | 1,9302-a 2-c | Lin et al., 1998 |
| 892-a | 3712-a | Showalter et al., 1996 | |
| 543 | 1,940 | Felder et al., 1995 | |
| 71.72-a 2-b | 2792-a 2-b | Hillard et al., 1999 | |
| 2522-b | 581 | Mechoulam et al., 1995 | |
| 2-Arachidonoylglycerol | 4722-b | 1,400 | Mechoulam et al., 1995 |
| 58.32-d | 1452-d | Ben-Shabat et al., 1998 | |
| HU-210 | 0.0608 | 0.524 | Felder et al., 1995 |
| 0.12-b | 0.17 | Rhee et al., 1997 | |
| 0.73 | 0.22 | Showalter et al., 1996 | |
| CP55940 | 5 | 1.8 | Ross et al., 1999a |
| 3.72 | 2.55 | Felder et al., 1995 | |
| 1.372-b | 1.372-b | Rinaldi-Carmona et al., 1994 | |
| 0.58 | 0.69 | Showalter et al., 1996 | |
| 0.502-a 2-b | 2.802-a 2-b | Hillard et al., 1999 | |
| Δ9-THC | 53.3 | 75.3 | Felder et al., 1995 |
| 39.52-b | 40 | Bayewitch et al., 1996 | |
| 40.7 | 36.4 | Showalter et al., 1996 | |
| 80.32-b | 32.2 | Rhee et al., 1997 | |
| 35.32-b | 3.92-b | Rinaldi-Carmona et al., 1994 | |
| Δ8-THC | 47.62-b | 39.32-c | Busch-Petersen et al., 1996 |
| R-(+)-WIN55212 | 9.942-b | 16.22-b | Rinaldi-Carmona et al., 1994 |
| 4.42-a 2-b | 1.22-a 2-b | Hillard et al., 1999 | |
| 1.89 | 0.28 | Showalter et al., 1996 | |
| 62.3 | 3.3 | Felder et al., 1995 | |
| 123 | 4.1 | Shire et al., 1996a | |
| CB2-selective ligands in order of increasing CB2/CB1 selectivity | |||
| JWH-015 | 383 | 13.8 | Showalter et al., 1996 |
| JWH-051 | 1.22-b | 0.032 | Huffman et al., 1996 |
| L-768242 | 1,917 | 12 | Gallant et al., 1996 |
| JWH-139 | 2,2902-b | 14 | Huffman et al., 1998 |
| AM 630 | 5,152 | 31.2 | Ross et al., 1999a |
| JWH-133 | 6772-b | 3.4 | Huffman et al., 1999 |
| L-759633 | 1,043 | 6.4 | Ross et al., 1999a |
| 15,850 | 20 | Gareau et al., 1996 | |
| L-759656 | 4,888 | 11.8 | Ross et al., 1999a |
| >20,000 | 19.4 | Gareau et al., 1996 | |
| HU-308 | >10,0002-b | 22.7 | Hanus et al., 1999 |
| SR144528 | 437 | 0.60 | Rinaldi-Carmona et al., 1998 |
| 3052-b | 0.302-b | Rinaldi-Carmona et al., 1998 | |
| >10,000 | 5.6 | Ross et al., 1999a | |
DMH, dimethylheptyl.
↵2-a With phenylmethylsulfonyl fluoride.
↵2-b Binding to rat cannabinoid receptors on transfected cells or on brain (CB1) or spleen tissue (CB2).
↵2-c Binding to mouse spleen cannabinoid receptors.
↵2-d Species unspecified. All other data from experiments with human cannabinoid receptors.