ar-9281 has been researched along with Inflammation* in 2 studies
2 other study(ies) available for ar-9281 and Inflammation
| Article | Year |
|---|---|
Movement to the Clinic of Soluble Epoxide Hydrolase Inhibitor EC5026 as an Analgesic for Neuropathic Pain and for Use as a Nonaddictive Opioid Alternative.
This report describes the development of an orally active analgesic that resolves inflammation and neuropathic pain without the addictive potential of opioids. EC5026 acts on the cytochrome P450 branch of the arachidonate cascade to stabilize epoxides of polyunsaturated fatty acids (EpFA), which are natural mediators that reduce pain, resolve inflammation, and maintain normal blood pressure. EC5026 is a slow-tight binding transition-state mimic that inhibits the soluble epoxide hydrolase (sEH) at picomolar concentrations. The sEH rapidly degrades EpFA; thus, inhibiting sEH increases EpFA Topics: Analgesics; Animals; Clinical Trials, Phase I as Topic; Dogs; Endoplasmic Reticulum Stress; Enzyme Inhibitors; Epoxide Hydrolases; Horses; Humans; Inflammation; Male; Molecular Structure; Neuralgia; Phenylurea Compounds; Rats, Sprague-Dawley; Structure-Activity Relationship | 2021 |
Design, synthesis and evaluation of non-urea inhibitors of soluble epoxide hydrolase.
Inhibition of soluble epoxide hydrolase (sEH) has been proposed as a new pharmaceutical approach for treating hypertension and vascular inflammation. The most potent sEH inhibitors reported in literature to date are urea derivatives. However, these compounds have limited pharmacokinetic profiles. We investigated non-urea amide derivatives as sEH inhibitors and identified a potent human sEH inhibitor 14-34 having potency comparable to urea-based inhibitors. Topics: Amides; Chemistry, Pharmaceutical; Drug Design; Enzyme Inhibitors; Epoxide Hydrolases; Fluorescent Dyes; Humans; Hydrogen Bonding; Hypertension; Inflammation; Inhibitory Concentration 50; Microscopy, Fluorescence; Models, Chemical; Solubility; Structure-Activity Relationship | 2012 |