Table 4.
Structures, chemical type and bioactivities of CB2-selective agonists.
Synthetic Cannabinoids | Chemical Type | Ki (nM)/CB | EC50 (nM)/CB2 | Bioactivity |
---|---|---|---|---|
![]() (a) JWH-133 |
Classical | 677/CB1 3.40/CB2 [104] |
63.0 [105] | Attenuating neurodegenerative and spatial memory impairment [27]; improving cerebral infarction [106]; anti-inflammatory, ameliorating sepsis [107]; anti-cancer [53]; anti-nociceptive [108]; protective effects on renal ischemia-reperfusion injury [109] and against cardiotoxicity [110] |
![]() (b) JWH-015 |
Amino-alkylindole | 383/CB1 13.8/CB2 [104] |
NA | Attenuating neurodegenerative, neuroprotective [106]; immunomodulatory, anti-inflammatory [53]; anti-nociceptive [111]; anti-cancer [112]; anti-obesity [25] |
![]() (c) PM-226 |
Classical | >40,000/CB1 12.8/CB2 [95] |
38.7 [95] | Neuroprotective [95]; anti-neuroinflammatory [78] |
![]() HU-308 |
Nonclassical | >10,000/CB1 22.7/CB2 [66] |
5.57 [23] | Anti-convulsant, neuroprotective [106]; anti-inflammatory [96,97]; anti-nociceptive [96]; anti-dyskinesia [98]; osteoprotective [97]; alleviating septic lung injury [113] |
![]() (e) GW-405833 |
Amino-alkylindole | 4772/CB1 3.92/CB2 [24] |
0.650 [24] | Anti-nociceptive, anti-inflammatory [99]; protective effects on acute liver injury [114] |
![]() (f) L-759,633 |
Classical | 1043, 15850/CB1 6.40, 20.0/CB2 [66] |
8.10 [115] | Analgesic [53] |
![]() (g) L-759,656 |
Classical | 529~>20000/CB1 11.8~57.0 [66] |
3.10 [115] | Analgesic [53] |
Ki: binding constant; EC50: half-maximal effective concentration; NA: not available.