TABLE 1

List of CB2 receptor ligand families and their structure-based classification (for agonists) examined in this study

ClassRepresentative Members
Classic cannabinoidsΔ9THC, L759633, L759656, JWH133, KM233
Nonclassic cannabinoidsCP55940, HU308
AminoalkylindolesWIN55212-2, AM1241,STS135, JWH015, GW405833, UR144, MAM2201, AM2232, AM2233, AM1248
ThiazolesA836339
Tricyclic pyrazoleGP1a
CannabilactoneAM1710
CarboxamidesSER601, 4Q3C
Pyrimidine analogGW833972A
Eicosanoids2AG, methanandamide
Plant products4-Methylhonokiol, (E) β-caryophyllene (BCP)
AntagonistsAM630, JTE907, SR144528
  • 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; BCP, (1R,4E,9S)-4,11,11-trimethyl-8-methylidenebicyclo[7.2.0]undec-4-ene; GP1a, N-(piperidin-1-yl)-1-(2,4-dichlorophenyl)-1,4-dihydro-6-methylindeno[1,2-c]pyrazole-3-carboxamide; GW405833, 1-(2,3-dichlorobenzoyl)-5-methoxy-2-methyl-3- [2-(4-morpholinyl)ethyl]-1H-indole; 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; JWH133, (6aR,10aR)-3-(1,1-Dimethylbutyl)-6a,7,10,10a-tetrahydro-6,6,9-trimethyl-6H-dibenzo[b,d]pyran; JWH015, (2-methyl-1-propyl-1H-indol-3-yl)-1-naphthalenylmethanone; 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; SER601, N-(Adamant-1-yl)-6-isopropyl-4-oxo-1-pentyl-1,4-dihydroquinoline-3-carboxamide Δ9THC, (−)-trans9-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; UR144, (1-pentyl-1H-indol-3-yl)(2,2,3,3-tetramethylcyclopropyl)-methanone.