GAT211 is an agonist and positive allosteric modulator (PAM) of cannabinoid receptor 1 (CB1) and a racemic mixture of GAT228 (Item No. 24485) and GAT229 (Item No. 24486), which have enantiomer-specific activities.1 GAT211 increases β-arrestin recruitment and cAMP inhibition in HEK293A cells expressing GFP-tagged human CB1 (hCB1-GFP) in a concentration-dependent manner. It also enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing hCB1, as well as the activity of 2-arachidonoyl glycerol (2-AG; Item No. 62160), arachidonoyl ethanolamide (AEA; Item No. 90050), and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. It inhibits excitatory postsynaptic currents (EPSCs) in a subset of CB1-expressing murine autaptic hippocampal neurons when used at a concentration of 1 µM.2 GAT211 also decreases mechanical hypersensitivity in wild-type (EC50 = 9.75 mg/kg), but not CB1 knockout, mice in a model of inflammatory pain induced by complete Freund’s adjuvant (CFA), and decreases mechanical and cold allodynia in a mouse model of paclitaxel-induced neuropathic pain when used at doses of 10 and 20 mg/kg per day.3WARNING This product is not for human or veterinary use.