Arachidonyl serotonin CAS NO.187947-37-1

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Arachidonyl serotonin is a dual target agent of transient receptor potential vanilloid-type I (TRPV1) antagonist and fatty acid amide hydrolase (FAAH) inhibitor, which is responsible for inactivation of anandamide and other endogenous cannabinoids. Its IC50 values are 37-40 nM and 5.6 μM for TRPV1 and FAAH respectively. It inhibits the FAAH activity isolated from mouse neuroblastoma cells with an IC50 value of 12 μM. It is a very tight binding, competitive inhibitor of FAAH. It does not inhibit cPLA2 and is essentially devoid of cannabimimetic activity. It was shown to be present in the ileum and jejunum of the gastrointestinal tract and modulate glucagon-like peptide-1 (GLP-1) secretion. It displays strong analgesic activity against both acute and chronic peripheral pain in rodents.