Table 2

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

LigandCB1KiValueCB2Ki ValueReference
CB1-selective ligands in order of decreasing CB1/CB2 selectivity
 ACEA1.42-a 2-b >2,0002-a 2-b Hillard et al., 1999
 O-18123.42-b 3,8702-b Di Marzo et al., 2001a
 SR141716A11.813,200 Felder et al., 1998
11.8973 Felder et al., 1995
12.3702 Showalter et al., 1996
5.6>1,000 Rinaldi-Carmona et al., 1994
1.982-b >1,0002-b Rinaldi-Carmona et al., 1994
 AM281122-b 4,2002-c Lan et al., 1999a
 ACPA2.22-a 2-b 7152-a 2-b Hillard et al., 1999
 2-Arachidonylglyceryl ether21.22-b >3,000 Hanus et al., 2001
 LY32013514114,900 Felder et al., 1998
R-(+)-methanandamide17.92-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
 Anandamide612-a 2-b 1,9302-a 2-c Lin et al., 1998
892-a 3712-a Showalter et al., 1996
5431,940 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-Arachidonoylglycerol4722-b 1,400 Mechoulam et al., 1995
58.32-d 1452-d Ben-Shabat et al., 1998
 HU-2100.06080.524 Felder et al., 1995
0.12-b 0.17 Rhee et al., 1997
0.730.22 Showalter et al., 1996
 CP5594051.8 Ross et al., 1999a
3.722.55 Felder et al., 1995
1.372-b 1.372-b Rinaldi-Carmona et al., 1994
0.580.69 Showalter et al., 1996
0.502-a 2-b 2.802-a 2-b Hillard et al., 1999
 Δ9-THC53.375.3 Felder et al., 1995
39.52-b 40 Bayewitch et al., 1996
40.736.4 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-THC47.62-b 39.32-c Busch-Petersen et al., 1996
R-(+)-WIN552129.942-b 16.22-b Rinaldi-Carmona et al., 1994
4.42-a 2-b 1.22-a 2-b Hillard et al., 1999
1.890.28 Showalter et al., 1996
62.33.3 Felder et al., 1995
1234.1 Shire et al., 1996a
CB2-selective ligands in order of increasing CB2/CB1 selectivity
 JWH-01538313.8 Showalter et al., 1996
 JWH-0511.22-b 0.032 Huffman et al., 1996
 L-7682421,91712 Gallant et al., 1996
 JWH-1392,2902-b 14 Huffman et al., 1998
 AM 6305,15231.2 Ross et al., 1999a
 JWH-1336772-b 3.4 Huffman et al., 1999
 L-7596331,0436.4 Ross et al., 1999a
15,85020 Gareau et al., 1996
 L-7596564,88811.8 Ross et al., 1999a
>20,00019.4 Gareau et al., 1996
 HU-308>10,0002-b 22.7 Hanus et al., 1999
 SR1445284370.60 Rinaldi-Carmona et al., 1998
3052-b 0.302-b Rinaldi-Carmona et al., 1998
>10,0005.6 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.