GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.

CB2:63 nM(EC50)

GW842166X demonstrates comparable potency and efficacy for rat and human recombinant CB2 receptors, with EC50 values of 91 nM and 63 nM, respectively. [1] It exhibits full agonist activity in cyclase assays with an EC50 of 133 nM and an Emax of 101%, and weak agonist activity in FLIPR assays with an EC50 of 7.780 μM and an Emax of 84%. [2]

GW842166X has an oral bioavailability of 58% and a half-life of 3 h when dosed orally in the rat. GW842166X has extremely high potency with an oral ED50 of 0.1 mg/kg and shows full reversal of hyperalgesia at 0.3 mg/kg in the FCAa model of inflammatory pain. [1] GW842166X orally administrated at a dose of 15 mg/kg for 8 days produced a significant reversal of the CCI induced decrease in paw withdrawal threshold in a rat model of neuropathic pain. [3]