GAT211, aslo known as AZ-4, is a small molecule CB1 positive allosteric modulator. GAT211 suppresses allodynia and produces synergistic antiallodynic effects with fatty acid amide hydrolase and monoacylglycerol lipase inhibitors in paclitaxel-treated mice. Positive allosteric modulation of CB1-receptor signaling with GAT211shows promise as a safe and effective analgesic strategy that lacks tolerance, dependence, and abuse liability.