非甾体抗炎药-血清素共轭物对脂肪酸酰胺水解酶、瞬时受体电位香草酸亚型1和环氧化酶2的抑制作用。
Inhibition of FAAH, TRPV1, and COX2 by NSAID-serotonin conjugates.
作者信息
Rose Tyler M, Reilly Christopher A, Deering-Rice Cassandra E, Brewster Clinton, Brewster Chelsea
机构信息
Roseman University of Health Sciences, College of Pharmacy, 10920 South River Front Parkway, South Jordan, UT 84095, USA.
University of Utah, College of Pharmacy, Department of Pharmacology and Toxicology, Salt Lake City, UT 84112, USA.
出版信息
Bioorg Med Chem Lett. 2014 Dec 15;24(24):5695-5698. doi: 10.1016/j.bmcl.2014.10.064. Epub 2014 Oct 28.
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.
摘要
血清素通过酰胺化作用与一系列结构多样的非甾体抗炎药（NSAIDs）的羧酸基团相连。对所得的NSAID - 血清素缀合物进行体外测试，以检测它们抑制脂肪酸酰胺水解酶（FAAH）、瞬时受体电位香草酸亚型1（TRPV1）和环氧化酶2（COX2）的能力。布洛芬 - 5 - 羟色胺（Ibuprofen - 5 - HT）和氟比洛芬 - 5 - 羟色胺（Flurbiprofen - 5 - HT）对这三个靶点的抑制能力与N - 花生四烯酰血清素（AA - 5 - HT）大致相同，而非诺洛芬 - 5 - 羟色胺（Fenoprofen - 5 - HT）和萘普生 - 5 - 羟色胺（Naproxen - 5 - HT）表现出作为TRPV1和COX2双重抑制剂的活性。
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