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A1480LS is a peripherally biased inhibitor of diacylglycerol lipase α (DAGLα) and DAGLβ (IC50s = 6 and 4 nM, respectively, in human brain membrane homogenates).1 It reduces levels of the DAGL-derived endocannabinoid 2-arachidonoyl glycerol (2-AG) in peripheral tissue but not in the brain in mice when administered at 20 mg/kg. A1480LS (20 mg/kg, p.o.) reduces mechanical allodynia in rat models of inflammatory pain and chemotherapy-induced neuropathy without inducing CNS adverse effects in the Irwin primary observation test.
WARNING This product is not for human or veterinary use.
1. Suppression of pain transmission and behavior by inhibition of peripheral diacylglycerol metabolism. Cell Chem. Bio. 33(1), 74-90.e19 (2025).