tcsc0854 AM630

AM630 is a selective CB₂ antagonist with K_i of 31.2 nM, and displays 165-fold selectivity over CB₁ receptors.

IC50 & Target: Ki: 31.2 nM (CB₂)

In Vitro: The AM251 and AM630-evoked Ca²⁺ influxes into TG sensory neurons aere concentration-dependent, and fitted. The EC₅₀ for AM251 and AM630 are 7.37 μM and 15.6 μM, respectively. AM251 and AM630 activate TRPA1 in TG sensory neurons. AM630 is comparable in value in both TRPA1 and TRPV1/TRPA1 expressing CHO cells (2 and 4.6 μM, respectively). AM251 and AM630 activation of TRPA1 is modulated by TRPV1^[2]. AM630 (0, 50, 100, and 200 nM) is not toxic to RAW264.7 cells. AM630 (100 nM) substantially inhibits osteoclastogenesis in cultures with RANKL and Ti particles in a dose-dependent manner^[3]. AM630 (1 μM) blocks the CP-55,940 dose response with EC₅₀ of 170 nM at human and EC₅₀ of 110 nM at rat cannabinoid CB2 receptor^[4].

In Vivo: AM630 (2, 3 mg/kg, i.p.) significantly reduces the time spent in the light box compared with vehicle group. AM630 increases anxiety since the time spent in the light box is reduced compared with its corresponding control group. 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^[1].