TABLE 3.
Transduction ratios and BFs of CB2 receptor ligands (cyclase over arrestin pathway)
| Compound | cAMP |
Arrestin |
|||||
|---|---|---|---|---|---|---|---|
| Log R | Δ Log(τ/KA) | Log R | Δ Log(τ/KA) | ΔΔ Log (τ/KA) | BF | 95% CI | |
| CP55940 | 8.10 | 0.00 | 8.27 | 0.00 | 0.00 | 1.00 | 0.95–1.08 |
| THC | 8.23 | 0.13 | 6.88 | −1.39 | 1.52 | 33.11 | 28.3–35.6 |
| L759633 | NA | NA | NA | NA | NA | NA | NA |
| L759656 | NA | NA | NA | NA | NA | NA | NA |
| JWH133 | 7.1 | −1 | 7 | −1.62 | 0.62 | 4.16 | 3.99–4.27 |
| KM233 | 8.73 | −0.04 | 7.1 | −1.52 | 1.48 | 30.19 | 28.19–33.56 |
| HU308 | 10.5 | 2.00 | 9.1 | 0.4 | 1.6 | 39.8 | 38.1–42.3 |
| WIN55212-2 | 8.9 | 0.867 | 8.22 | −0.007 | 0.874 | 7.41 | 5.8–8.7 |
| AM1241 | 7.73 | −0.46 | 6.8 | −1.9 | 1.44 | 27.54 | 24.9–31.6 |
| STS135 | 7.88 | −0.62 | 8.79 | 0.05 | −0.67 | 0.2 | 0.14–0.29 |
| JWH015 | 8.56 | 0.363 | 7.65 | −1.09 | 1.45 | 28.13 | 26.1–32.9 |
| GW405833 | NA | NA | NA | NA | NA | NA | NA |
| UR144 | 7.9 | −0.8 | 10.5 | 2 | −2.8 | 0.0015 | 0.0007–0.002 |
| MAM2201 | 8.25 | −0.32 | 10.1 | 1.36 | 1.68 | 47.86 | 41.4–56.1 |
| AM2232 | 8.34 | 0.09 | 7.0 | −1.23 | 1.32 | 20.89 | 16.2-28.7 |
| AM2233 | NA | NA | NA | NA | NA | NA | NA |
| AM1248 | 7.39 | −1.2 | 8.78 | 0.04 | −1.16 | 0.079 | 0.043–0.12 |
| A836339 | 9.1 | 0.4 | 9.1 | 0.32 | 0.08 | 1.2 | 0.91–1.7 |
| GP1a | 7.8 | −0.7 | 7.95 | −0.75 | 0.05 | 1.12 | 0.4–1.9 |
| AM1710 | 7.92 | −0.33 | 7.919 | −0.358 | −0.028 | 0.95 | 0.5–1.2 |
| SER601 | 8.85 | 0.35 | 7.04 | −1.23 | 1.58 | 38.01 | 30.2–45.7 |
| 4Q3C | NA | NA | NA | NA | NA | NA | NA |
| GW833972A | 7.65 | −0.85 | 7.37 | −1.25 | 0.4 | 2.5 | 1.7–2.9 |
| 2AG | 8.393 | 0.290 | 6.9 | −1.37 | 1.66 | 47.8 | 45.2–51.1 |
| Meth-anandamide | 9.67 | 1.1 | 7.51 | −0.381 | 1.5 | 32 | 30.51–35.78 |
| 4 Methylhonokiol | 7 | −1.103 | 10.010 | 1.733 | −2.836 | 0.002 | 0.0014–0.032 |
| β Caryophyllene | NA | NA | NA | NA | NA | NA | NA |
| AM630 | NA | NA | NA | NA | NA | NA | NA |
| JTE907 | NA | NA | NA | NA | NA | NA | NA |
| SR144528 | NA | NA | NA | NA | NA | NA | NA |
AM1241, (2-iodo-5-nitrophenyl)-(1-(1-methylpiperidin-2-ylmethyl)-1H-indol-3-yl)methanone; AM1248, 1-[(N-methylpiperidin-2-yl)methyl]-3-(adamant-1-oyl)indole; AM2232, (1-(4-cyanobutyl)-3-(naphthalen-1-oyl)indole); A836339, N-[3-(2-methoxyethyl)-4,5-dimethyl-1,3-thiazol-2-ylidene]-2,2,3,3-tetramethylcyclopropane-1-carboxamide; GP1a, N-(piperidin-1-yl)-1-(2,4-dichlorophenyl)-1,4-dihydro-6-methylindeno[1,2-c]pyrazole-3-carboxamide; GW833972A, 2-[(3-chlorophenyl)amino]-N-(4-pyridinylmethyl)-4-(trifluoromethyl)-5-pyrimidinecarboxamide hydrochloride; HU308, 4-[4-(1,1-dimethylheptyl)-2,6-dimethoxyphenyl]-6,6-dimethylbicyclo[3.1.1]hept-2-ene-2-methanol; JTE907, N-(1,3-benzodioxol-5-ylmethyl)-1,2-dihydro-7-methoxy-2-oxo-8-(pentyloxy)-3-quinolinecarboxamide; JWH015, (2-methyl-1-propyl-1H-indol-3-yl)-1-naphthalenylmethanone; JWH133, (6aR,10aR)-3-(1,1-Dimethylbutyl)-6a,7,10,10a-tetrahydro-6,6,9-trimethyl-6H-dibenzo[b,d]pyran; KM233, (−)-(6aR,7,10,10aR)-tetrahydro-6,6,9-trimethyl-3-(1-methyl-1-phenylethyl)-6H-dibenzo[b,d]pyran-1-ol; L759633, (6aR,10aR)-1-methoxy-6,6,9-trimethyl-3-(2-methyloctan-2-yl)-6a,7,10,10a-tetrahydrobenzo[c]chromene; L759656, (6aR,10aR)-3-(1,1-dimethylheptyl)-6a,7,8,9,10,10a-hexahydro-1-methoxy-6,6-dimethyl-9-methylene-6H-dibenzo[b,d]pyran; MAM2201, [1-(5-fluoropentyl)-1H-indol-3-yl](4-methyl-1-naphthalenyl)-methanone; NA, not applicable/cannot be determined; SER601, N-(Adamant-1-yl)-6-isopropyl-4-oxo-1-pentyl-1,4-dihydroquinoline-3-carboxamide; THC, tetrahydrocannabinol; 4Q3C, 1,4-dihydro-8-methoxy-4-oxo-1-pentyl-N-tricyclo[3.3.1.13,7]dec-1-yl-3-quinolinecarboxamide; WIN55212-2, [(3R)-2,3-dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-naphthalenyl-methanone, monomethanesulfonate.