AM 1172 is a potent and selective inhibitor of anandamide uptake and FAAH.
Metabolically stable anandamide uptake inhibitor (IC 50 = 2.1 - 2.5 μ M) and fatty acid amide hydrolase (FAAH) inhibitor (K i = 3.18 μ M). Inhibits N -arachidonylethanolamine (AEA) accumulation (IC 50 = 24 μ M) and hydrolysis (K i = 3 μ M), and inhibits N -palmitoylethanolamine (PEA) hydrolysis (IC 50 = 36 μ M) in cerebellar granule neurons. Also acts as a non-selective cannabinoid receptor partial agonist (EC 50 values are 189 and 271 nM at CB 2 and CB 1 receptors respectively).
1. fegley d, kathuria s, mercier r, et al. anandamide transport is independent of fatty-acid amide hydrolase activity and is blocked by the hydrolysis-resistant inhibitor am1172. proceedings of the national academy of sciences of the united states of america. 2004;101(23):8756-8761.
