SA 57

SA 57 is an inhibitor of fatty acid amide hydrolase (FAAH; IC₅₀s = 1.9 and 3.2 nM for hFAAH and mFAAH, respectively), monoacylglycerol lipase (MAGL; IC₅₀s = 1,400 and 410 nM for hMAGL and mMAGL, respectively) and α/β-hydrolase domain-containing protein 6 (mABHD6; IC₅₀ = 850 nM).¹ In vivo, SA 57, at doses ≥1.25 mg/kg, selectively inactivates mFAAH and, at a dose of 12.5 mg/kg, inactivates mMAGL and mABHD6 resulting in a 10-fold increase in their substrates. Administration of SA 57 (5 mg/kg, i.p.) to morphine-dependent mice alleviates withdrawal signs without eliciting cannabimimetic side effects.²

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1. Niphakis, M.J., Johnson, D.S., Ballard, T.E., et al. O-hydroxyacetamide carbamates as a highly potent and selective class of endocannabinoid hydrolase inhibitors. ACS Chem Neurosci. 3(5), 418-426 (2012).

2. Ramesh, D., Gamage, T.F., Vanuytsel, T., et al. Dual inhibition of endocannabinoid catabolic enzymes produces enhanced antiwithdrawal effects in morphine-dependent mice. Neuropsychopharmacology 38(6), 1039-1049 (2013).