mast cells

Mizolastine (SL 850324) (IC50= 47 nM) is a histamine H1-receptor antagonist.It is used in the treatment of allergic reactions such as hay fever (seasonal allergic rhinitis), hives.

Pimecrolimus (SDZ-ASM 981), a calcineurin inhibitor immunosuppressant, binds to the receptor macrophilin-12 (FKBP-12) forming a complex that blocks the calcium-dependent signal transduction cascade mediated by calcineurin.

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.

Nylidrin hydrochloride (Buphenine HCl) was an effective inhibitor of the IgG1-mediated release of histamine from passively sensitized guinea pig lung slices, and of the IgE-mediated release of histamine from passively sensitized rat peritoneal mast cells and human basophils.

Salbutamol (Albuterol) stimulates beta2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of ATP to cyclic-3', 5'-adenosine monophosphate (cAMP). Salbutamol Sulfate is the sulfate salt of the short-acting sympathomimetic agent albuterol, a 1:1 racemic mixture of (R)-albuterol and (S)-albuterol with bronchodilator activity. Increased cAMP concentrations relax the bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. To a lesser extent, Salbutamol stimulates beta1-adrenergic receptors, thereby increasing the force and rate of myocardial contraction.

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

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

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.

1-Heptanol (Heptan-1-ol) is a RIFM spice that is a cell membrane fluidizer and induces signaling to mast cells.1-Heptanol shows antiarrhythmic effects in atrial species of Langendorff perfused mouse hearts.1-Heptanol is a RIFM spice that is a cell membrane fluidizer and induces signaling to mast cells.1-Heptanol is a RIFM spice that is a RIFM spice and induces signaling to mast cells.

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

MK-571 sodium (L-660711 sodium salt) is a selective, orally active antagonist of the CysLT1 receptor. MK-571 sodium is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics, and their conjugates. MK-571 sodium can inhibit the synthesis of K-4′-O-GlcA (19.7 μM). MK571 dose-dependently inhibits the intracellular biosynthesis of all flavonol sulphates and glucuronides by Caco-2 cells. MK-571 sodium significantly inhibits phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-4′-O-glucuronide was competitively inhibited. In addition to inhibiting MRP2, MK571 is a potent inhibitor of enterocyte phase-2 conjugation.

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

WHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal.

PKC ζ pseudosubstrate acetate is an inhibitor of protein kinase C (PKC) ζ; attached to cell permeabilisation Antennapedia domain vector peptide. Consists of amino acids 113 - 129 of PKC ζ pseudosubstrate domain linked by a disulphide bridge to the Antenna

GSK-5498A is a selective blocker of CARC (IC50, 1 μM). It inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.

Pemirolast Potassium is the potassium salt form of pemirolast, a pyrimidinone derivative with antiallergic property. Pemirolast potassium (TWT-8152) exerts its action by blocking the antigen-mediated calcium ion influx into mast cells.

Tazanolast, a selective mast-cell-stabilizing drug, inhibits the release of chemical mediators (histamine and leukotrienes) from mast cells, reduces inflammation, and is used in the treatment of allergic disorders, such as asthma and allergic rhinitis.

Nedocromil sodium is a pharmacologic stabilizer of mast cells, has been shown to normalize cytokine levels and attenuate cardiac remodeling.

8 Hydroxy PIPAT oxalate is a selective 5-HT1A receptor agonist that enhances the spontaneous release of histamine by promoting the degranulation of mast cells in guinea pig and human intestinal preparations. By activating the serotonin signaling pathway, this compound demonstrates potential in regulating gastrointestinal functions and offers insight into the management and suppression of functional gastrointestinal disorders such as irritable bowel syndrome. Its effects in increasing histamine release could play a crucial role in gastrointestinal regulation.

Torososide B is an anti-allergic compound that inhibits leukotriene release from calcium ionophore A-stimulated rat peritoneal mast cells.

JNJ 10191584 maleate (VUF6002 maleate) is an orally active and selective antagonist of H4 receptor (Ki = 26 nM). JNJ 10191584 maleate inhibits chemotaxis of eosinophils and mast cells (IC50 = 530 nM and 138 nM).

A1777, a selective 5-lipoxygenase inhibitor, reduces leukocytes proliferation without affecting the eosinophils of mast cells.

Tiaramide hydrochloride (FK-1160) is an anti-inflammatory drug that inhibits the action of mediators released from mast cells and has direct smooth muscle relaxant properties.

TEI-9063 is a stable and highly specific prostacyclin analogue of prostacyclin receptor in mast cell tumor p-815 cells.