DO34 is a selective and potent diacylglycerol lipase (DAGL-α/β) inhibitor that impairs fear extinction in mice, and can be used to study lipopolysaccharide inflammatory pain.

DAGLβ:3-8 nM, DAGLα:6 nM

DO34 is a potent, selective and centrally active DAGL inhibitor, the efficiency of DAGLα in converting SAG to 2-AG was determined by a real-time fluorescence-based natural substrate assay using membrane lysates from HEK293T cells expressing recombinant human DAGLα, DAGLα IC50 = 6 nM.DO34 is also a potent DAGLβ inhibitor, DAGLβ DO34 is also a potent DAGLβ inhibitor, DAGLβ IC50 = 3-8 nM. [1]

DO34 reduces 2-AG levels in the brain in a dose- and time-dependent manner and prevents fasting-induced regurgitation in mice, which is typical of cannabinoid CB1 receptor-mediated behavior, and DO34 blocks tonic CB1 activation.DO34 blocks basal PF-EPSCs in AM251-increased MAGL-TKO mice. [2]