TABLE 1

Characterization of compounds in radioligand competition binding assays using [3H]CP 55,940


Ligands

Mean Ki (nM)*, 95% Confidence Interval of Ki Values (nM)
hCB2
hCB1
hCB2/hCB1 Selectivity
rCB2
rCB1
rCB2/rCB1 Selectivity
A-836339 0.64 270 421 0.76 143 189
0.46–0.90 130–590 0.42–1.3 66–310
A-796260 4.6 950 206 16 400 26
2.2–9.6 580–1500 9.2–26 170–900
JWH-015 35 1200 34 63 770 12
27–46 760–1900 40–97 490–120
AM1241 10 1300 125 3.4 120 36
6.8–16 350–4500 1.6–7.3 7.7–1700
GW-842166X 2000 >10000 N.A. 2600 >10,000 N.A.
560–7100 990–6700
L-768,242 (GW405833) 7.6 1600 210 11 N.D. N.A.

2.2–26
1100–2500

4.7–26


  • N.D., not determined; N.A., not applicable

  • * All Ki values are derived from at least three studies performed in duplicate