allergic disease

PF-03654746 is a selective antagonist of the histamine H3 receptor. PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease. PF-03654746 can be used in studies about the treatment of allergic rhinitis.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

Etosalamide (Ethosalamide) is an antipyretic and analgesics agent.

Diphenylpyraline hydrochloride (4-Diphenylmethoxy-1-methylpiperidine hydrochloride) is used in the treatment of Parkinsonism.It is a first-generation antihistamine with anticholinergic effects, functions as a dopamine reuptake inhibitor.

COX 5-LO-IN-1 is a cyclooxygenase and 5-lipoxygenase (5-LO) inhibitor, and used for inflammatory and allergic disease states.

NPC 567 acetate is a bradykinin B2 antagonist and can be used in studies about the treatment of allergic airway disease.

4-DAMP (4-DAMP methiodide) is a selective muscarinic M1 and M3 subtype receptor antagonist used in the study of allergic rhinitis and cardiovascular disease.

Andolast, also known as CR-2039, an anti-allergic agent for the treatment of bronchial asthma, chronic obstructive pulmonary disease (COPD). Andolast acts at different cellular levels to inhibit immunoglobulin E synthesis. Andolast proved to be significan

CP-664511 is an alpha4beta1/ vascular cell adhesion molecule-1 (VCAM-1) inhibitor with therapeutic potential for allergic airway disease.

PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50= 31 nM).1It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer's disease.4 1.March, D.R., Proctor, L.M., Stoermer, M.J., et al.Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activityMol. Pharmacol.65(4)868-879(2004) 2.Jain, U., Woodruff, T.M., and Stadnyk, A.W.The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10Br. J. Pharmacol.168(2)488-501(2013) 3.Staab, E.B., Sanderson, S.D., Wells, S.M., et al.Treatment with the C5a receptor/CD88 antagonist PMX205 reduces inflammation in a murine model of allergic asthmaInt. Immunopharmacol.21(2)293-300(2014) 4.Fonseca, M.I., Ager, R.R., Chu, S.-H., et al.Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's diseaseJ. Immunol.183(2)1375-1383(2009)

TR-14035 (MDK-1191) is a dual antagonist of α4β7 α4β1 integrins (IC50s: 7 87nM).

Sequifenadine has the potential in researching of inflammatory eye disease with allergic symptoms that is a H1-antihistamine [1] [2].

Adriforant tartrate hydrate, also known as ZPL-3893787 tartrate hydrate, PF-3893787 tartrate hydrate and ZPL-389 tartrate hydrate, is a novel histamine H4 receptor antagonist. Adriforant tartrate hydrate shows an excellent in vitro profile that warrants their further investigation in relevant models of human disease. Histamine H4 receptor (H4R) has become a promising target for immuno-inflammatory diseases, such as allergic rhinitis, asthma or dermal allergies.

PM-43I is a potent inhibitor of both STAT5- and STAT6-dependent allergic airway disease in mice.

Theophylline-d6 is intended for use as an internal standard for the quantification of theophylline by GC- or LC-MS. Theophylline is an inhibitor of phosphodiesterase. It is also an adenosine A1 and A2 receptor antagonist. Theophylline induces relaxation of isolated cat bronchial smooth muscle segments precontracted with acetylcholine. It inhibits ovalbumin-induced increases in bronchoalveolar lavage fluid (BALF) eosinophil infiltration in an ovalbumin-sensitized mouse model of allergic asthma. Formulations containing theophylline have been used in the treatment of asthma and chronic obstructive pulmonary disease (COPD).

Nerandomilast (BI 1015550) is an orally active PDE4B inhibitor with IC50 of 7.2 nM. BI 1015550 has potential applications in inflammation, allergic diseases, pulmonary fibrosis and chronic obstructive pulmonary disease (COPD) with a good safety profile.

STAT6-IN-1, a STAT6 inhibitor, exhibits high affinity for the SH2 domain of STAT6 (IC 50 = 0.028 µM), making it suitable for research on allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease, or cancer.

PM-81I, a potent STAT6 inhibitor targeting the SH2 structural domain, effectively reduces STAT6 phosphorylation levels. It is applicable in the research of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease, or cancer [1].

Maceneolignan H (Compound 8), a neolignane derived from the arils of Myristica fragrans, acts as a selective CCR3 antagonist with an EC 50 value of 1.4 μM. This compound shows promise for allergic disease research [1].

EPI-X4, an endogenous peptide fragment of human serum albumin (amino acids 408-423), serves as an antagonist to the chemokine (C-X-C motif) receptor 4 (CXCR4). It effectively prevents calcium mobilization and receptor internalization triggered by chemokine (C-X-C motif) ligand 12 (CXCL12) in HEK293 cells with CXCR4 expression, at concentrations between 0.8 and 1,000 µM. Moreover, EPI-X4 hampers the CXCL12-driven migration of both Jurkat T cells and human CD34+ hematopoietic stem cells. In an acute allergic airway hypereosinophilia mouse model, EPI-X4 intrinsically decreases Cxcr4-dependent inflammatory cell infiltration in airways at a dose of 16 µmol/kg. Additionally, increased urinary EPI-X4 levels, inversely related to glomerular filtration rate (GFR), are observed in chronic kidney disease patients, indicating its potential biomarker role.

(±)9(10)-DiHOME, the diol derivative of (±)9(10)-EpOME—a cytochrome P450-derived epoxide of linoleic acid also known as leukotoxin—is formed through the action of soluble epoxide hydrolase (sEH) in neutrophils. It exhibits toxicity towards Sf21 cells expressing sEH as well as tolacZ-expressing control cells, differing from leukotoxin which only harms sEH-containing cells. Furthermore, combined exposure to 9(10)- and 12(13)-DiHOME leads to cell death in rabbit renal proximal tubule cells by disrupting mitochondrial respiration, and causes lung injury, respiratory distress, and mortality in mice, highlighting its role as a toxic lipid mediator. Specifically, 9(10)-DiHOME has been associated with acute respiratory distress syndrome (ARDS), a severe and often deadly complication in patients with major burns. Elevated levels of this compound have been detected in the bronchoalveolar lavage fluid (BALF) of women, but not men, with chronic obstructive pulmonary disease (COPD), and its levels are also increased in patients with allergic asthma, indicating its significance in respiratory conditions.

Ayanin has vasorelaxant activity, it also may have the potential for use in treating allergic asthma.The IC(50) value of Ayanin (quercetin-3,7,4'-O-trimethylether) is 2.2microM for inhibiting interleukin (IL)-4 production from purified basophils.

1,6-O,O-Diacetylbritannilactone(OODBL) has anti-inflammatory activity, it has a potential therapeutic efficacy on inflammatory diseases especially allergic airway disease as a lead compound. OODBL has anti-asthmatic activity, it reduces leukotriene C4 pro

TAT-N15, a p55PIK inhibitor, demonstrates significant anti-inflammatory and neuroprotective effects. It effectively suppresses the activation of IL-6, IL-8, Akt, and NF-κB pathways, along with the phosphorylation of STAT3 and the protein expression of NF-κB. TAT-N15 is applicable for research on acute conjunctivitis, allergic rhinitis, chronic obstructive pulmonary disease (COPD), and stroke through its inhibition of Akt, STAT3, and NF-κB pathways.