SAR127303 is an orally active, selective, competitive monoacylglycerol lipase ( MAGL ) covalent inhibitor with IC 50 s of 3.8 nM and 29 nM for mouse and human MAGL , respectively. SAR127303 potently elevates hippocampal levels of 2-AG in mice. SAR127303 decreased long term potentiation (LTP) of CA1 synaptic transmission and acetylcholine release in the hippocampus. SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. SAR127303 slows down epileptogenesis.
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