Potent, selective cellular uptake inhibitor of anandamide (IC50 = 4.9 μM in primary culture). Able to inhibit FAAH (Ki = 9.7 μM). Poor affinity for CB1 and CB2 receptors (Ki = 5 and >10 μM, respectively) and no activity at vannilloid VR1 receptors (EC50 = >10 μM).
Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Soluble in ethanol and DMSO to 50 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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Hillard CJ et al. Studies of anandamide accumulation inhibitors in cerebellar granule neurons: comparison to inhibition of fatty acid amide hydrolase. J Mol Neurosci33:18-24 (2007).
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de Lago E et al. In vivo pharmacological actions of two novel inhibitors of anandamide cellular uptake. Eur J Pharmacol484:249-57 (2004).
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Ortar G et al. Novel selective and metabolically stable inhibitors of anandamide cellular uptake. Biochem Pharmacol65:1473-81 (2003).
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