GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC 50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research
In Vitro
GAT211 is stable in both human- and rat-liver microsomal incubations, with t 1/2 of 28.4 min and 8.67 min, repsectively. GAT211 limits dopamine D2 receptor-mediated extracellular regulated kinase (ERK) phosphorylation in Neuro2a cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GAT211 potentiates the inhibition of electrically evoked vas deferens contraction in the same system (EC 50 =11 nM, E max =70). GAT211 (0.3 mg/kg, 1 mg/kg, 3 mg/kg; 5 mL/kg; ip; 2 doses with 5 min interval) dose-dependently reduced locomotor activity and the acoustic startle response.GAT211 is dissolved in a vehicle of ethanol, kolliphor, and saline at a ratio of 1:1:6 and injected at a volume of 5 mL/kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
