• Bioorg. Med. Chem. Lett. · Dec 2014

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

    • Tyler M Rose, Christopher A Reilly, Cassandra E Deering-Rice, Clinton Brewster, and Chelsea Brewster.
    • Roseman University of Health Sciences, College of Pharmacy, 10920 South River Front Parkway, South Jordan, UT 84095, USA. Electronic address: trose@roseman.edu.
    • Bioorg. Med. Chem. Lett. 2014 Dec 15;24(24):5695-8.

    AbstractSerotonin 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.Copyright © 2014 Elsevier Ltd. All rights reserved.

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