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  • ||||||||||  Disopain (mofezolac) / Mitsubishi Tanabe
    Biomarker, Journal:  Targeting COX-1 by mofezolac-based fluorescent probes for ovarian cancer detection. (Pubmed Central) -  Nov 6, 2019   
    Fingerprints for Ligands and Proteins (FLAP) software calculations were performed to justify 11 higher COX-1 inhibitory potency than mofezolac (COX-1 IC = 5.1 nM), which in turn is a moiety of 11. Specifically, the two compounds bind differently in the COX-1 active site.
  • ||||||||||  ibuprofen / generics
    Journal:  Cox-2 inhibitors in mandibular third molar surgery. (Pubmed Central) -  Oct 19, 2019   
    The new Cox-2 selective inhibitors, or coxibs, show the same anti-inflammatory, analgesic, and antipyretic effects as nonselective NSAIDs but are supposed to have reduced side-effect profiles. This study evaluates whether rofecoxib (50 mg) given one hour pre-operatively or the same drug given one hour post-operatively is more effective in controlling the pain and swelling in mandibular third molar surgery.
  • ||||||||||  celecoxib oral / Generic Mfg.
    Modulation of the Inflammatory Response Benefits Treatment-Resistant Bipolar Depression (Floridian Ballroom) -  Oct 17, 2019 - Abstract #ACNP2019ACNP_261;    
    Furthermore, the results of this study, in spite of the relatively small sample size, suggest that the use of CBX as adjunctive medication could reverse treatment resistance in patients with TRBDD in a safe and effective manner. This supports the clinical potential of anti-inflammatory agents for adjunctive treatment and more effective management of mood disorders.
  • ||||||||||  Journal:  Protease-activated receptor 2 protects against myocardial ischemia-reperfusion injury through the lipoxygenase pathway and TRPV1 channels. (Pubmed Central) -  Oct 12, 2019   
    Nordihydroguaiaretic acid (a general LOX inhibitor) and baicalein (a 12-LOX inhibitor), but not indomethacin (a cyclooxygenase inhibitor) and hexanamide (a selective cytochrome P450 epoxygenase inhibitor), abolished the protective effects of SLIGRL in WT (all P<0.05) but not in TRPV1 hearts. These data suggested that PAR2, possibly via 12-LOX, activates TRPV1 and leads to CGRP and substance P release to prevent I/R injury in the heart, indicating that the 12-LOX-TRPV1 pathway conveys cardiac protection to alleviate myocardial infarction.
  • ||||||||||  piroxicam / generics
    Preclinical, Journal:  Unique regulation of Na-glutamine cotransporter SN2/SNAT5 in rabbit intestinal crypt cells during chronic enteritis. (Pubmed Central) -  Oct 12, 2019   
    After 2-week incubation, control and inflamed rabbits were subjected to intramuscular injections of arachidonyl trifluoromethyl ketone (ATK), piroxicam and MK886 for 48 hrs...COX inhibition proved ineffective at reversing the stimulation of SN2. Thus, this study provides evidence that SN2 stimulation in crypt cells is mediated by the leukotriene pathway during chronic intestinal inflammation.
  • ||||||||||  Journal:  Decidual stromal cell-derived PGE regulates macrophage responses to microbial threat. (Pubmed Central) -  Oct 10, 2019   
    Thus, this study provides evidence that SN2 stimulation in crypt cells is mediated by the leukotriene pathway during chronic intestinal inflammation. These data suggest key roles for decidual stromal cells in modulating tissue responses to microbial threat through release of PGE .
  • ||||||||||  Journal, Cancer stem cells:  A reactive oxygen species-generating, cancer stem cell-potent manganese(ii) complex and its encapsulation into polymeric nanoparticles. (Pubmed Central) -  Oct 8, 2019   
    Notably, the manganese(ii) complex, 1, exhibits 9-fold, 31-fold, and 40-fold greater potency towards breast CSCs than 3, salinomycin (an established breast CSC-potent agent), and cisplatin (a clinically approved anticancer drug) respectively...The nanoparticle formulation 1 NP indiscriminately kills breast CSCs and bulk breast cancer cells, and evokes a similar cellular response to the payload, 1. To the best of our knowledge, this is the first study to investigate the anti-CSC properties of managense complexes and to demonstrate that polymeric nanoparticles can be used to effectively deliver managense complexes into CSCs.
  • ||||||||||  Desoxyn (methamphetamine) / Lundbeck
    Journal:  Methamphetamine-Induced Brain Injury and Alcohol Drinking. (Pubmed Central) -  Oct 4, 2019   
    Cyclooxygenase inhibition by ketoprofen during EtOH drinking blocked the increases in LPS and COX-2 and the enhanced decreases in dopamine and serotonin produced by Meth. Therefore, prior EtOH drinking causes an increase in inflammatory mediators that mediate a synergistic interaction with Meth to cause an enhanced neurotoxicity.
  • ||||||||||  Journal:  Targeting the COX/mPGES-1/PGE Pathway in Neuroblastoma. (Pubmed Central) -  Oct 3, 2019   
    Prostaglandin E is formed from its precursor arachidonic acid in a two-step enzymatic reaction. Arachidonic acid is first converted by cyclooxygenases into prostaglandin H and then further converted by microsomal prostaglandin E synthase-1 into prostaglandin E. We believe targeting of microsomal prostaglandin E synthase-1 in cancer-associated fibroblasts will be an effective future therapeutic strategy in fighting neuroblastoma.
  • ||||||||||  Tamoxis (tamoxifen) / Bioprofarma, Dynastat (parecoxib) / Pfizer, celecoxib oral / Generic Mfg.
    Journal:  Cyclooxygenase-2, Asymmetric Dimethylarginine and the Cardiovascular Hazard from NSAIDs. (Pubmed Central) -  Sep 30, 2019   
    The Bcl-2 inhibitors combined with CART cells might even enhance the cytotoxic effect. Analysis of the plasma and renal metabolome was performed in postnatal tamoxifen-inducible Cox-2 knockout mice, which exhibit normal renal function and blood pressure...Therapeutic concentrations of the selective COX-2 inhibitors, rofecoxib, celecoxib, and parecoxib, none of which altered basal blood pressure or renal function as reflected by plasma creatinine, failed to elevate plasma arginine and methylarginines in mice...Conclusions-Plasma methylarginines are not altered by COX-2 deletion or inhibition but rather are elevated coincident with renal compromise.
  • ||||||||||  Journal:  1,8-Cineole blocks voltage-gated L-type calcium channels in tracheal smooth muscle. (Pubmed Central) -  Sep 28, 2019   
    In conclusion, 1,8-cineole has a dual effect on tracheal smooth muscle contraction resulting in a biphasic effect. Our data suggest that the potentiation effect is mediated by activation of TRPM8 channels and the relaxation effect is mediated by the blockage of L-type VGCC.
  • ||||||||||  celecoxib oral / Generic Mfg.
    Journal:  Can a cyclooxygenase inhibitor be an option for treatment of ovarian hyperstimulation syndrome? (Pubmed Central) -  Sep 28, 2019   
    After treatment, however, a significant difference was observed only between group 2 and the other groups (P=0.001, P=0.002, P=0.038). According to these results, celecoxib significantly decreased VEGF, IL-2, and ET-1 levels as much as cabergoline and could reduce the extent of OHSS development.
  • ||||||||||  Clinical, Review, Journal:  Prospective for cytochrome P450 epoxygenase cardiovascular and renal therapeutics. (Pubmed Central) -  Sep 26, 2019   
    Novel small molecules that inhibit sEH have advanced to human clinical trials and demonstrate promise for cardiovascular diseases. Challenges remain for sEH inhibitor and EET analog drug development; however, there is a high likelihood that a drug that acts on this third branch of arachidonic acid metabolism will be utilized to treat a cardiovascular or kidney disease in the next decade.
  • ||||||||||  NSAID use and breast cancer risk in a retrospective cohort of women with benign breast disease (Hall 1 - Poster Session 5) -  Sep 25, 2019 - Abstract #SABCS2019SABCS_718;    
    Conclusions In this exploratory analysis, we found use of ibuprofen and other NSAIDs to be associated with decreased BC risk among women who had undergone a BBD biopsy. These findings suggest that anti-inflammatory approaches may have value in chemoprevention among women with BBD.
  • ||||||||||  semaxanib (SU5416) / Pfizer
    Journal, PD(L)-1 Biomarker, IO Biomarker:  A Dominant Role for Regulatory T Cells in Protecting Females Against Pulmonary Hypertension. (Pubmed Central) -  Sep 22, 2019   
    Male and female athymic rnu/rnu rats, lacking Tregs, were treated with the VEGFR2 (vascular endothelial growth factor receptor 2) inhibitor SU5416 or chronic hypoxia and evaluated for PH; some animals underwent Treg immune reconstitution before SU5416 administration...In vitro, human Tregs directly upregulated endothelial COX-2, PDL1, HO-1, ERs and increased supernatant levels of PGI2 and IL-10.In two animal models of PH based on Treg deficiency, females developed more severe PH than males. The data suggest that females are especially reliant on normal Treg function to counteract the effects of pulmonary vascular injury leading to PH.
  • ||||||||||  celecoxib oral / Generic Mfg.
    Journal:  Celecoxib alleviates nonalcoholic fatty liver disease by restoring autophagic flux. (Pubmed Central) -  Sep 20, 2019   
    Western blot and RFP-GFP-LC3 double fluorescence system indicated that celecoxib could ameliorate steatosis and restore autophagic flux in L02 cells treated with palmitate as well as SD rats fed with high-fat diet. In conclusion, celecoxib partially restores autophagic flux via downregulation of COX-2 and alleviates steatosis in vitro and in vivo.
  • ||||||||||  ibuprofen / generics
    Journal:  Effect of antibiotics and NSAIDs on cyclooxygenase-2 in the enamel mineralization. (Pubmed Central) -  Sep 20, 2019   
    Groups treated with amoxicillin, amoxicillin/clavulanate, erythromycin and acetaminophen showed significantly lower amounts of immunoreactive COX2 at the enamel organ maturation stage of the mouse incisors. Our results suggest that COX2 is involved in the maturation stage of the enamel organ and that its inhibition would appear to alter amelogenesis, producing hypomineralization.
  • ||||||||||  aspirin / Generic Mfg.
    Journal:  Residual cyclooxygenase activity of aspirin-acetylated COX-2 forms 15 R-prostaglandins that inhibit platelet aggregation. (Pubmed Central) -  Sep 20, 2019   
    We conclude that acetylation of Ser530 in COX-2 not only triggers formation of 15 R-HETE but also allows oxygenation and cyclization of arachidonic acid to a 15 R-PG endoperoxide. 15 R-PGs are novel products of aspirin therapy via acetylation of COX-2 and may contribute to its antiplatelet and other pharmacologic effects.-Giménez-Bastida, J. A., Boeglin, W. E., Boutaud, O., Malkowski, M. G., Schneider, C. Residual cyclooxygenase activity of aspirin-acetylated COX-2 forms 15 R-prostaglandins that inhibit platelet aggregation.
  • ||||||||||  dexamethasone / generics
    PK/PD data, Preclinical, Journal:  Assessing Drug Interaction and Pharmacokinetics of Loxoprofen in Mice Treated with CYP3A Modulators. (Pubmed Central) -  Sep 19, 2019   
    Therefore, we investigated the metabolism of LOX after pretreatment with dexamethasone (DEX) and ketoconazole (KTC), which induce and inhibit the activities of CYP3A, respectively...The opposite result occurred with KTC (a CYP3A inhibitor) pretreatment. Thus, we conclude that concomitant use of LOX with CYP3A modulators may lead to drug-drug interactions and result in minor to severe toxicity even though there is no direct change in the metabolic pathway that forms the LOX active metabolite.
  • ||||||||||  aspirin / Generic Mfg.
    Journal:  Entamoeba histolytica Cyclooxygenase-Like Protein Regulates Cysteine Protease Expression and Virulence. (Pubmed Central) -  Sep 12, 2019   
    ...Live virulent Eh pretreated with arachidonic acid substrate to enhance PGE production or aspirin to inhibit EhCox enzyme activity or addition of exogenous PGE to Eh had no effect on EhCP activity...This study has identified EhCox protein as one of the important endogenous regulators of cysteine protease activity. Alterations of CP activity in response to Cox gene silencing may be a negative feedback mechanism in Eh to limit proteolytic activity during colonization that can inadvertently trigger inflammation in the gut.
  • ||||||||||  glibenclamide / generics
    Journal:  Vasorelaxant effect of sinensetin via the NO/sGC/cGMP pathway and potassium and calcium channels. (Pubmed Central) -  Sep 8, 2019   
    Sinensetin was also active in reducing Ca release from the sarcoplasmic reticulum (via IPR) and in blocking calcium channels (VOCC). The present study demonstrates the vasorelaxant effect of sinensetin, which involves the NO/sGC/cGMP and indomethacin pathways, calcium and potassium channels, and muscarinic and beta-adrenergic receptors.
  • ||||||||||  Journal:  Guaianolides from Ormenis mixta: Structural Insights and Evaluation of Their Anti-inflammatory Profile. (Pubmed Central) -  Sep 7, 2019   
    The isolates were assayed for their anti-inflammatory potential evaluating nitric oxide release and cyclooxygenase-2 expression in J774A.1 macrophages treated with lipopolysaccharide from Escherichia coli. Our results indicated that, among the tested compounds, 1:  - 3: , and 7: were able to inhibit nitric oxide release, while all were able to inhibit cyclooxygenase-2 expression with different potencies.
  • ||||||||||  Avandia (rosiglitazone) / GSK
    Journal:  Design, synthesis, modeling studies and biological evaluation of thiazolidine derivatives containing pyrazole core as potential anti-diabetic PPAR-γ agonists and anti-inflammatory COX-2 selective inhibitors. (Pubmed Central) -  Sep 6, 2019   
    Also, two thiazolidindione derivatives 12e and 12f and two thiazolidinone derivatives 13b and 13c showed higher inhibitory activities against α- and β-glucosidase (% inhibitory activity = 62.15, 55.30, 65.37, 59.08 for α-glucosidase and 57.42, 60.07, 58.19, 66.90 for β-glucosidase respectively) than reference compounds (acarbose with % inhibitory activity = 49.50 for α-glucosidase and d-saccharic acid 1,4-lactone monohydrate with % inhibitory activity = 53.42 for β-glucosidase) and also showed good PPAR-γ activation and good hypoglycemic effect in comparison to pioglitazone and rosiglitazone. Moreover, Shape comparison and docking studies were carried out to understand their interaction and similarity with standard drugs.