allergy

Diphenhydramine (Syntedril), a first-generation antihistamine possessing antiemetic, antitussive, anticholinergic, and sedative properties, is mainly used in the treatment of allergies. Diphenhydramine is also used in the management of drug-induced parkinsonism and other extrapyramidal symptoms.

Tecastemizole (R 43512) is a selective antagonist of H1 receptor and a major metabolite of astemizole with anti-inflammatory effects.

Fexofenadine (Carboxyterfenadine), an antihistamine pharmaceutical drug, is used to treat allergy symptoms, such as nasal congestion, hay fever, and urticaria. Compared to first-generation antihistamines, Fexofenadine is less able to pass the blood-brain barrier and cause sedation.

2-Bromo-4'-hydroxyacetophenone(PTP Inhibitor I) is a cell-permeable, protein tyrosine phosphatase (PTP) inhibitor that covalently blocks the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)) with a Ki value of 43 μM and PTP1B with a Ki value of 42 μM [1]. SHP-1 and PTP1B both have known roles in regulating insulin signaling as well as myeloid and lymphoid cell differentiation, making inhibitors of these phosphatases of interest in diabetes, cancer, allergy, and inflammation research [2].

Evatanepag (CP-533536 free acid) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

SCH-336 is a CB2 receptor agonist (Ki-1.8 nM, EC50-2 nM) with effective, selective, and oral activity. SCH-336 is also bioactive against CB1 receptor, and is 100 times more selective to CB2 receptor than CB1. SCH-336 reduced the binding of guanosine 5' -3-o -(sulfur) triphosphate to the membrane containing hCB, inhibited BaF3 CB2 cell migration, inhibited leukocyte migration in mouse delayed hypersensitivity models, and inhibited antigen-induced pulmonary eosinophilia in mouse allergy models.

Cinfenoac is a derivative of chalcone. This compound is used to treat inflammation and allergy symptoms, as well as gastrointestinal ulcers.

YFJ-36 is an antibiotic that demonstrates superior and broad-spectrum antibacterial activity in vitro compared to cefiderocol, particularly against A. baumannii and K. pneumoniae. In a systemic infection model in mice, YFJ-36 exhibits strong in vivo efficacy. Additionally, the compound shows enhanced physicochemical stability in liquid media with a pH of 6-8 and is noteworthy for its potential to reduce allergy risk due to its quaternary ammonium bond.

A 78773 is a potent, selective, direct, and reversible 5-lipoxygenase inhibitor. It has activity in a variety of purified cells and in more complex biological systems such as whole blood, lung fragments, and tracheal tissues. A 78773 acts against inflamma

PF-06462894 is a morpholinopyrimidone mGlu5 (mGlu5 Ki = 6 nM) with favorable properties. PF-06462894 did not show any evidence of immune activation in a mouse drug allergy model.

Acamelin is a quinone isolated from the Australian black wood acacia melanoxylon. It is responsible for the allergy-inducing properties of the species.

Setipiprant (ACT-129968) is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2, a G protein-coupled receptor for prostaglandin (PGD2), mediates key inflammatory responses related to allergy and asthma. PGD2, produced by mast cells, binds to CRTH2 on blood-borne cells, inducing chemotaxis of Th2 cells, basophils, and eosinophils, and stimulating cytokine release.

Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminomethyl)benzamide) is the analogue of BMS-509744, which can potently and selectively inhibit Itk kinase activity. In vitro: BMS-509744 could reduce TCR-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells [1]. In vivo: BMS-509744 suppressed the production of IL-2 induced by anti-TCR antibody administered to mice. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma [1]. Clinical trial: Up to now, both BMS-509744 and ITK inhibitor is still in the preclinical development stage.

Secoxyloganin possesses a hepato-protective effect. Secoxyloganin possesses antibacterial activity. Secoxyloganin has cytotoxic activity against UACC-62 cell line.Secoxyloganin possesses the perfect protective effect on PRRSV infected cell and with the minimum protection concentration of 6. 25 μg mL.

AHR-5333 mandelate is an anti-allergy compound which has been shown to protect against antigen-induced anaphylactic collapse and ascaris antigen-induced skin hypersensitivity. AHR-5333 mandelate has also been shown to inhibit 5-HETE, LTB4 and LTC4 synthesis.

OVA Peptide (323-339) is an immunodominant epitope peptide derived from chicken ovalbumin (OVA), which is the major MHC class II-restricted T-cell epitope that specifically binds H2-IAd molecules, and a B-cell epitope that is recognized by IgE antibodies. It is commonly used in the study of egg allergy, and is able to induce strong Th2-type immune responses and IgE antibody production in mice.

ER-27319, an acridone derivative, serves as a potent and selective inhibitor of spleen tyrosine kinase (SYK), effectively impeding both the tyrosine phosphorylation and enzymatic activity of SYK. With an inhibitory concentration (IC50) of 10 µM, this compound suppresses the release of allergic mediators from human and rat mast cells triggered by antigens, making it useful for allergy research [1] [2].

17-Hydroxyneomatrine, a compound derived from Sophora flavescens, exhibits multifaceted biological activities, including the inhibition of human cervical carcinoma Hela cell growth, along with broad-spectrum antibacterial, anti-allergy, anti-tumor, anti-arrhythmia, diuretic, anti-inflammatory, immunomodulatory, and bio-regulatory properties [1].

Ovalbumin (OVA) peptide, primarily found in egg white, is a class I (Kb)-restricted peptide epitope presented by H-2Kb, the mouse MHC (major histocompatibility complex) class I gene product. It has garnered significant attention in the field of allergy research [1] [2].

Gomisin N, isolated from Schisandra chinensis, exhibits sedative and hypnotic bioactivity. It has potential applications in allergy treatment and inhibits proliferation while inducing apoptosis in cancer cells.

BTL-MK (Compound 19) is an orally active antiallergic agent that inhibits degranulation of mast cells with an IC50 of 6.7 μM by binding to the inhibitory receptor FcγRIIB. BTL-MK improves metabolic stability in human liver microsomes and ameliorates the allergic response in an Ovalbumin-induced food allergy mice model. It exhibits good pharmacokinetic characteristics with metabolic stability [1].

RWJ-58643 is a β-trypsin and trypsin inhibitor used in studies to inhibit allergic inflammatory conditions. The compound was effective in reducing nasal allergy symptoms, eosinophil infiltration, and interleukin-5 (IL-5) levels at a lower dose (100 mg). However, at higher doses (300 mg and 600 mg), an increase in eosinophils and elevated IL-5 levels were observed, showing a clear dose-dependent response.

Spiraeoside (Quercetin 4′-O-glucoside) is a compound that can be extracted from red onion skins. It exhibits antioxidant, anti-allergy, anti-inflammatory, and anti-tumor activities. It protects human myocardial cells from high glucose-induced damage, oxidative stress, and apoptosis by activating the PI3K Akt Nrf2 pathway. It also inhibits mast cell activation and IgE-mediated allergic reactions by suppressing phospholipase C-γ-mediated signaling.

Uvaol is present in olives and virgin olive oil with anti-inflammatory, anti-proliferative, and vasorelaxant activities.