GAT211

GAT211 is an agonist and positive allosteric modulator (PAM) of cannabinoid receptor 1 (CB1) and a racemic mixture of GAT228 (Cay-24485) and GAT229 (Cay-24486), which have enantiomer-specific activities. GAT211 increases beta-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, Cay-62160), arachidonoyl ethanolamide (AEA, Cay-90050), and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCbeta3 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. 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.Formal Name: 3-(2-nitro-1-phenylethyl)-2-phenyl-1H-indole. CAS Number: 102704-40-5. Molecular Formula: C22H18N2O2. Formula Weight: 342.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 10 mg/ml, Ethanol: 5 mg/ml. lambdamax: 300 nm. SMILES: O=[N+](CC(C1=CC=CC=C1)C2=C(C3=CC=CC=C3)NC4=CC=CC=C42)[O-]. InChi Code: InChI=1S/C22H18N2O2/c25-24(26)15-19(16-9-3-1-4-10-16)21-18-13-7-8-14-20(18)23-22(21)17-11-5-2-6-12-17/h1-14,19,23H,15H2. InChi Key: OHZDCJJHWPHZJD-UHFFFAOYSA-N.