Literature DB >> 25467164

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

Tyler M Rose1, Christopher A Reilly2, Cassandra E Deering-Rice2, Clinton Brewster3, Chelsea Brewster3.   

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.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Arachidonoyl serotonin; Dual inhibition; FAAH; Fatty acid amide hydrolase; Multimodal inhibition; NSAID; TRPV1; Transient receptor potential vanilloid type 1

Mesh：

Substances：

Year:  2014        PMID： 25467164      PMCID： PMC4258163          DOI： 10.1016/j.bmcl.2014.10.064

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  41 in total

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