TABLE 1.

Some K_i values of cannabinoid CB₁/CB₂ receptor ligands for the in vitro displacement of a tritiated compound^a from specific binding sites on rat, mouse, or human CB₁ and CB₂ receptors

Unless otherwise indicated in the Reference column, see Pertwee, 2005a for references. Structures of the compounds listed are shown in Figs. 1 to 5.

Cannabinoid Receptor Ligand	Ki		Reference
	CB1	CB2
	nM
Section II.C.1
(−)-Δ9-THC	5.05–80.3	3.13–75.3	See Pertwee, 2008a for references
HU-210	0.06–0.73	0.17–0.52
CP55940	0.5–5.0	0.69–2.8
R-(+)-WIN55212	1.89–123	0.28–16.2
Anandamide	61–543	279–1940
2-AG	58.3, 472	145, 1400
Section II.C.2
Agonists with higher CB1 than CB2 affinity
ACEA	1.4, 5.29	195, >2000
Arachidonylcyclopropylamide	2.2	715
R-(+)-methanandamide	17.9–28.3	815–868
Noladin ether	21.2	>3000
Agonists with higher CB2 than CB1 affinity
JWH-133	677	3.4
HU-308	>10000	22.7
JWH-015	383	13.8
AM1241	280	3.4
Section II.C.3
Rimonabant (SR141716A)	1.8–12.3	514–13,200
AM251	7.49	2290
AM281	12	4200
LY320135	141	14,900
Taranabant	0.13, 0.27	170, 310	Fong et al., 2007
NESS 0327	0.00035	21
O-2050	2.5, 1.7	1.5	Martin et al., 2002; A. Thomas and R. G. Pertwee, unpublished data
Section II.C.4
SR144528	50.3–>10,000	0.28–5.6
AM630	5152	31.2
JTE-907	2370	35.9
Section II.C.5
11-OH-Δ8-THC	25.8	7.4
Ajulemic acid	5.7, 32.3	56.1, 170.5	Dyson et al., 2005; see also Pertwee, 2005a, for references
Cannabinol	120–1130	96–301	See Pertwee, 2008 for references
Cannabigerol	81	2600	Cascio et al., 2010
Cannabidiol	4350–>10,000	2399–>10,000	See Pertwee, 2008 for references
N-Arachidonoyl dopamine	250	12,000	Bisogno et al., 2000
Virodhamine	912	N.D.	Steffens et al., 2005

N.D., no data.

^aUsually [³H]CP55940, but sometimes [³H]SR141716A, [³H]R-(+)-WIN55212, or HU-243 (i.e., [³H]HU-210).