Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: Inhibition of FAAH, TRPV1, and COX2 by NSAID-serotonin conjugates.

Authors: Tyler M Rose, Christopher A Reilly, Cassandra E Deering-Rice, Clinton Brewster, Chelsea Brewster

Journal, date & volume: Bioorg. Med. Chem. Lett., 2014 Dec 15 , 24, 5695-8

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/25467164

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.