AM 1172

Biological Activity

Metabolically stable anandamide uptake inhibitor (IC₅₀ = 2.1 - 2.5 μM) and fatty acid amide hydrolase (FAAH) inhibitor (K_i = 3.18 μM). Inhibits N-arachidonylethanolamine (AEA) accumulation (IC₅₀ = 24 μM) and hydrolysis (K_i = 3 μM), and inhibits N-palmitoylethanolamine (PEA) hydrolysis (IC₅₀ = 36 μM) in cerebellar granule neurons. Also acts as a non-selective cannabinoid receptor partial agonist (EC₅₀ values are 189 and 271 nM at CB₂ and CB₁ receptors respectively). FABP inhibitor.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Anandamide uptake is consistent with rate-limited diffusion and is regulated by the degree of its hydrolysis by fatty acid amide hydrolase.
   Kaczocha et al.
   J.Biol.Chem., 2006;281:9066
2. Studies of anandamide accumulation inhibitors in cerebellar granule neurons.
   Hillard et al.
   J.Mol.Neurosci., 2007;33:18
3. Anandamide transport is independent of fatty-acid amide hydrolase activity and is blocked by the hydrolysis-resistant inhibitor AM1172.
   Fegley et al.
   Proc.Natl.Acad.Sci.USA, 2004;101:8756
4. A personal retrospective: Elevating Anandamide (AEA) by targeting fatty acid amide hydrolase (FAAH) and the fatty acid binding proteins (FABPs).
   Deutsch
   Front.Pharmacol., 2017;7:370

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