Formulation: A solid
Formal Name: 3-[(1R)-2-nitro-1-phenylethyl]-2-phenyl-1H-indole
Purity: ≥98%
Formula Markup: C22H18N2O2
Formula Weight: 342,4
Shelf life (days): 1460
CAS Number: 1446648-15-2
Notes: GAT228 is an allosteric agonist of cannabinoid receptor 1 (CB1), the R-(+)-enantiomer of the CB1 positive allosteric modulator (PAM) GAT229 (Item No. 24486), and a component of the racemic mixture GAT211, which acts as both an agonist and PAM.{35179,48089} GAT228 increases β-arrestin recruitment, cAMP inhibition, and ERK1/2 and PLCβ3 phosphorylation in HEK293A cells expressing GFP-tagged human CB1 (hCB1-GFP) in a concentration-dependent manner.{35179} Unlike GAT229, GAT228 has no effect on the binding of the CB receptor agonist CP 55,940 to membranes from CHO cells expressing hCB1 when used at concentrations up to 1 µM. It inhibits excitatory postsynaptic currents (EPSCs) in a subset of CB1-expressing murine autaptic hippocampal neurons when used at a concentration of 1 µM.{48089}