Potent, selective and irreversible inhibitor of MAG lipase (IC50=8nM vs 4µM for FAAH). JZL-184-treated mice displayed a number of CB1-dependent behavioral effects including analgesia, hypothermia and hypomotility as well as increased levels of 2-arachidonoylglycerol in the brain ( approx. 8-fold, with no effect on anandamide levels). JZL-184 produces a rapid and sustained blockade of brain 2-AG hydrolase activity in mice. It blocks neuropathic pain and enhances retrograde endocannabinoid signaling.
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