期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 24, 页码 5695-5698出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.10.064
关键词
NSAID; FAAH; Fatty acid amide hydrolase; TRPV1; Transient receptor potential vanilloid type 1; Dual inhibition; Multimodal inhibition; Arachidonoyl serotonin
资金
- National Institutes of Health, National Institute of Environmental Health Sciences [ES017431]
- NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES [R01ES017431] Funding Source: NIH RePORTER
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. (C) 2014 Elsevier Ltd. All rights reserved.
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