Title: Inhibition of FAAH, TRPV1, and COX2 by NSAID-serotonin conjugates.
Authors: Rose, Tyler M; Reilly, Christopher A; Deering-Rice, Cassandra E; Brewster, Clinton; Brewster, Chelsea
Published In Bioorg Med Chem Lett, (2014 Dec 15)
Abstract: Serotonin was linked by amidation to the carboxylic acid groups of a series of structurally diverse NSAIDs. The resulting NSAID-serotonin conjugates were tested in vitro for their ability to inhibit FAAH, TRPV1, and COX2. Ibuprofen-5-HT and Flurbiprofen-5-HT inhibited all three targets with approximately the same potency as N-arachidonoyl serotonin (AA-5-HT), while Fenoprofen-5-HT and Naproxen-5-HT showed activity as dual inhibitors of TRPV1 and COX2.
PubMed ID: 25467164
MeSH Terms: Amidohydrolases/antagonists & inhibitors*; Anti-Inflammatory Agents, Non-Steroidal/chemistry*; Anti-Inflammatory Agents, Non-Steroidal/pharmacology*; Cyclooxygenase 2/chemistry*; Flurbiprofen/chemistry; Flurbiprofen/metabolism; Humans; Serotonin/chemistry*; Serotonin/metabolism; TRPV Cation Channels/antagonists & inhibitors*