164178-33-0

Ki: 31.2 nM (CB ₂ )

The AM251 and 6-Iodopravadoline (AM630)-evoked Ca ²⁺ influxes into TG sensory neurons aere concentration-dependent, and fitted. The EC ₅₀ for AM251 and 6-Iodopravadoline are 7.37 μM and 15.6 μM, respectively. AM251 and 6-Iodopravadoline activate TRPA1 in TG sensory neurons. 6-Iodopravadoline is comparable in value in both TRPA1 and TRPV1/TRPA1 expressing CHO cells (2 and 4.6 μM, respectively). AM251 and 6-Iodopravadoline activation of TRPA1 is modulated by TRPV1. 6-Iodopravadoline (0, 50, 100, and 200 nM) is not toxic to RAW264.7 cells. 6-Iodopravadoline (100 nM) substantially inhibits osteoclastogenesis in cultures with RANKL and Ti particles in a dose-dependent manner. 6-Iodopravadoline (1 μM) blocks the CP-55,940 dose response with EC ₅₀ of 170 nM at human and EC ₅₀ of 110 nM at rat cannabinoid CB2 receptor.

6-Iodopravadoline (AM630) (2, 3 mg/kg, i.p.) significantly reduces the time spent in the light box compared with vehicle group. 6-Iodopravadoline (AM630) (1, 2 or 3 mg/kg, i.p., twice a day) produces a significant anxiolytic effect, increasing the time spent in the light box at all of the doses used.