Peripheral FAAH and soluble epoxide hydrolase inhibitors are synergistically antinociceptive
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چکیده
منابع مشابه
Peripheral FAAH and soluble epoxide hydrolase inhibitors are synergistically antinociceptive.
We need better medicines to control acute and chronic pain. Fatty acid amide hydrolase (FAAH) and soluble epoxide hydrolase (sEH) catalyze the deactivating hydrolysis of two classes of bioactive lipid mediators--fatty acid ethanolamides (FAEs) and epoxidized fatty acids (EpFAs), respectively--which are biogenetically distinct but share the ability to attenuate pain responses and inflammation. I...
متن کاملSoluble epoxide hydrolase inhibitors and heart failure.
Cardiovascular disease remains one of the leading causes of death in the Western societies. Heart failure (HF) is due primarily to progressive myocardial dysfunction accompanied by myocardial remodeling. Once HF develops, the condition is, in most cases, irreversible and is associated with a very high mortality rate. Soluble epoxide hydrolase (sEH) is an enzyme that catalyzes the hydrolysis of ...
متن کاملOrally bioavailable potent soluble epoxide hydrolase inhibitors.
A series of N,N'-disubstituted ureas having a conformationally restricted cis- or trans-1,4-cyclohexane alpha to the urea were prepared and tested as soluble epoxide hydrolase (sEH) inhibitors. This series of compounds showed low nanomolar to picomolar activities against recombinant human sEH. Both isomers showed similar potencies, but the trans isomers were more metabolically stable in human h...
متن کاملDual Inhibitors of COX-2 and Soluble Epoxide Hydrolase (sEH)
A series of novel Dual Inhibitors of COX-2 and sEH containing an N-urea substituted pyrazole as a lead for sEH inhibition have been synthesized and screened as novel analogues to reduce blood pressure elevation by acting as sEH inhibitors. The synthesized compounds having varying degrees of selectivity towards the sEH enzymes. Particularly compounds 6g and 6i emerged as the most potent sEH inhi...
متن کاملDesign, Synthesis and Biological Activity of 4,6-disubstituted Pyridin-2(1H)-ones as Novel Inhibitors of Soluble Epoxide Hydrolase
Soluble epoxide hydrolase enzyme is a promising therapeutic target for hypertension, vascular inflammation, pain and some other risk factors of cardiovascular diseases. The most potent sEH inhibitors reported in the literature are urea-based ones which often have poor bioavailability. In this study, in a quest for finding potent inhibitors of soluble epoxide hydrolase, some 4,6-disubstituted py...
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ژورنال
عنوان ژورنال: Pharmacological Research
سال: 2015
ISSN: 1043-6618
DOI: 10.1016/j.phrs.2015.04.001