mediators

EC5026 (BPN-19186) has the potential to relieve pain by stabilizing natural analgesic and anti-inflammatory mediators.

1. 2,5-Dihydroxyacetophenone (Quinacetophenone) possess anti-anxiety, and neuroprotective qualities. 2. 2,5-Dihydroxyacetophenone (Quinacetophenone) reatment can induce a sustained activation of JNK, ERK1/2, and p38 MAPKs, it also can potentiate the pro-apoptotic and anti-proliferative effects of bortezomib in U266 cells. 3. 2,5-Dihydroxyacetophenone (Quinacetophenone) has anti-inflammatory activity in activated macrophages, raising the possibility that this compound has a therapeutic potential for inflammatory conditions. 4. 2,5-Dihydroxyacetophenone (Quinacetophenone) is an uncompetitive inhibitor of murine tyrosinase (K(I) 0.28mm), it strongly inhibits both melanogenesis and cellular tyrosinase activity in vitro in 3-isobutyl-1-methylxanthin-stimulated B16 mouse melanoma cells or in vivo in zebrafish and mouse models.

Deoxyandrographolide (14-deoxyandrographolide) potentiates NGF-induced neurite outgrowth. Deoxyandrographolide suppresses the production of proinflammatory mediators TNF-α and IL-6.

Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

Isoflupredone (Isoflupredonum) is a synthetic corticosteroid that acts in vivo by binding to glucocorticoid and corticosteroid receptors in animals (such as horses) to inhibit inflammatory cells and inhibit the expression of inflammatory mediators. Isoflupredone has anti-inflammatory and immunosuppressive effects and can be used to treat a variety of musculoskeletal, allergic and systemic inflammatory diseases.

Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor that reduces the production of pro-inflammatory mediators and cytokines. Dovramilast is used in the study of Mycobacterium tuberculosis infections and lupus erythematosus.

Navamepent (RX-10045) is an analog of resolvin E1 (a dietary-3 polyunsaturated fatty acid metabolite), which has potent anti-inflammatory activity that reduces corneal inflammation, epithelial damage, and accelerates corneal tissue repair.Navamepent inhibits the release of several key pro-inflammatory mediators from corneal epithelial cells.Navamepent is very effective against dry eye and cupping cell loss Navamepent is effective against dry eye and cupping cell loss, and accelerates tear production.

Cortisone Acetate is a synthetic or semisynthetic analog of the naturally occurring cortisone hormone produced by the adrenal glands with anti-inflammatory and immunomodulating properties. Cortisone acetate (NSC-49420) diffuses through the cell membrane and binds to nuclear glucocorticoid receptors. The receptor-ligand complex binds to promotor regions of certain genes and initiates RNA transcription. This results in an induction of synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators.

Budesonide (Pulmicort), an anti-inflammatory corticosteroid, has shown the effective glucocorticoid activitie and few mineralocorticoid activities. According to reports, Budesonide has extensively inhibitory effects against multiple cells types and mediators referred to allergic and nonallergic-mediated inflammatory. What's more, the anti-inflammatory action of budesonide has been revealed to contribute to the effectiveness of asthma.

Ketotifen fumarate (HC 20511 fumarate) is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators.

Desonide (Prednacinolone) is a synthetic glucocorticosteroid for topical use, with anti-inflammatory activity. Desonide binds to glucocorticoid receptors in the cytoplasm, and the ligand-receptor complex is translocated as a homodimer into the nucleus, where transcription activation via glucocorticoid response elements within glucocorticoid-responsive genes occur. This agent induces transcription of genes coding for anti-inflammatory proteins, including lipocortin-1, interleukin-10, interleukin-1 receptor antagonist and neutral endopeptidase. Increased synthesis of lipocortin-1 has an inhibitory effect on phospholipase A2, which in turn inhibits the release of arachidonic acid, thereby controlling the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Cromolyn sodium (FPL-670) is a chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells.

Betamethasone Dipropionate is the 17, 21-dipropionate ester of betamethasone, a synthetic glucocorticoid with metabolic, immunosuppressive and anti-inflammatory actions. Betamethasone dipropionate (SCH 11460) binds to specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. The synthesis of certain anti-inflammatory proteins is induced while the synthesis of certain inflammatory mediators is inhibited. As a result, there is an overall reduction in chronic inflammation and autoimmune reactions.

Clobetasol propionate (CGP9555) exerts its effect by binding to cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor-mediated gene expression. This results in the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Clobetasol Propionate is the propionate salt form of clobetasol, a topical synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. Specifically, clobetasol propionate appears to induce phospholipase A2 inhibitory proteins, thereby controlling the release of the inflammatory precursor arachidonic acid from membrane phospholipids by phospholipase A2.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK/p38 MAPK signaling pathways in the murine macrophages.

Arachidonic acid (Immunocytophyt) is a polyunsaturated omega-6 essential fatty acid that serves as a major component of biological membranes and animal phospholipids. It is synthesized from dietary linoleic acid and acts as a precursor to lipid mediators such as prostaglandins, thromboxanes, and leukotrienes. Arachidonic acid can improve cognitive responses and cardiovascular function and is commonly used to induce paw edema models.

Uridine-5'-diphosphate disodium salt (UDP disodium salt) is a specific agonist of the P2Y6 receptors (EC50 = 13 nM for human P2Y6), stimulating the production of inflammatory mediators, phagocytosis, and vasoconstriction. Uridine-5'-diphosphate disodium salt also acts as an antagonist of P2Y14.

Palmitoylethanolamide (Impulsin) is an endogenously fatty acid amide. It has a role as an anti-inflammatory drug, an antihypertensive agent, a neuroprotective agent and an anticonvulsant.Upon administration, palmitoylethanolamide may inhibit the release of pro-inflammatory mediators from activated mast cells.

Ethyl linoleate is a natural product.

MAO-B-IN-8 is a highly potent and reversible inhibitor of monoamine oxidase-B (MAO-B), also inhibiting microglial production of neuroinflammatory mediators. This compound is specifically designed for research on neurodegenerative diseases [1].

Triamcinolone (Aristocort) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.

Medrysone (6α-Methyl-11β-hydroxyprogesterone) is a topical, synthetic glucocorticoid with metabolic, anti-inflammatory and anti-allergic properties. Medrysone exerts its effect by interacting with specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. This results in an induction of the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Consequently, an overall reduction in chronic inflammation and autoimmune reactions is accomplished.

(E/Z)-BCI (NSC-150117), a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory properties, reduces LPS-induced inflammatory mediators and ROS production in macrophage cells by activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.

SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models.