rhinitis

Mometasone furoate (Sch32088) is a pregnadienediol derivative with anti-allergic and anti-inflammatory properties, used in the management of asthma and allergic rhinitis, as well as a topical treatment for skin disorders.

Ectoine (L-Ectoine) is an osmoprotectant in a variety of microorganisms including halophilic and heterotrophic bacteria and non-halophilic bacteria such as the Streptomyces species, as well as E.coli.

Rupatadine Fumarate (Rinialer) (UR-12592 Fumarate) is a potent dual PAF H1 antagonist with Ki of 0.55 0.1 uM.

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.

Ebastine (Kestine) (trade names Evastin, Kestine, Ebastel, Aleva) is a non-sedating H1 antihistamine. It does not penetrate the blood-brain barrier and thus allows an effective block of the H1 receptor in peripheral tissue without a central side effect, i. e not causing sedation or drowsiness.

Nafamostat mesylate (FUT-175), a synthetic serine protease inhibitor, has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.

Triprolidine hydrochloride monohydrate is a histamine H1 antagonist used in allergic rhinitis, asthma.

Fluticasone propionate (CCI-187881), derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.

Tripelennamine hydrochloride (Pyribenzamine hydrochloride) is a histamine H1 antagonist with low sedative action but frequent gastrointestinal irritation.

Cetirizine dihydrochloride (UCB P071) is an effective second-generation histamine H1 antagonist that is potent in the therapy of allergic rhinitis, confirmed urticaria, and pollen-induced asthma. Unlike other conventional antihistamines, it does not cause side effects of drowsiness or anticholinergic.

Ramatroban (BAY u3405) (BAY u3405) is a thromboxane A(2) (TxA(2)) antagonist marketed for allergic rhinitis. It has been used in trials studying the treatment of Asthma.

Tylosin tartrate, a macrolide antibiotic, is approved for the control of mycoplasmosis in poultry.

Tylosin (Tylosine) is a macrolide antibiotic obtained from cultures of Streptomyces fradiae. The drug is effective against many microorganisms in animals but not in humans.

Trans-Tranilast is an antiallergic drug developed by Kissei Pharmaceuticals. It was approved in 1982 for use in Japan and South Korea for bronchial asthma. Indications for keloid and hypertrophic scar were added in 1993. It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.

Ipratropium bromide monohydrate (Ipratropium bromide hydrate) is a muscarinic antagonist structurally related to ATROPINE but often considered safer and more effective for inhalation use. It is used for various bronchial disorders, in rhinitis, and as an antiarrhythmic.

Brompheniramine maleate (Dimotane) is an antagonist against histamine H1 receptors.

Cromoglicic acid prevents the release of inflammatory chemicals such as histamine from mast cells.

Azelastine (Azelastinum) is a phthalazine derivative, and is an histamine antagonist and mast cell stabilizer.

(2-{[2-(2-fluorophenoxy)ethyl]sulfanyl}-1H-benzimidazol-1-yl)acetic acid is a prostaglandin-like CRTH2 antagonist with an IC50 < 10 μM, which can be used in studies of rhinitis, COPD, rheumatoid arthritis, eczema and conjunctivitis.

mTOR HDAC-IN-1 (Compound 50) is a dual inhibitor of mTOR and HDAC, with IC50 values of 0.49 nM and 0.91 nM, respectively, holding potential as an anti-cancer agent [1].

AZD8848 is a selective antedrug agonist of toll-like receptor 7 (TLR7). It is developed for the research of asthma and allergic rhinitis.

5-A-RU (5-Amino-6-(D-ribitylamino)uracil), a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules that are derived from other metabolic pathways.This compound is unstable in powder form and other related salt forms are recommended.

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.

Bencycloquidium Bromide is a muscarinic M3 antagonist. Bencycloquidium bromide inhibits nasal hypersecretion in a rat model of allergic rhinitis. Bencycloquidium Bromide showed high affinity toward the M(3) receptor in Chinese hamster ovary (CHO) cells (M(1) pKi=7.86, M(2) pKi=7.21, M(3) pKi=8.21); pA(2)=8.85, 8.71 and 8.57 in methacholine-induced contraction of trachea, ileum and urinary bladder, 8.19 in methacholine-induced bradycardia of right atrium in vitro, respectively.This compound is unstable in powder form and other related salt forms are recommended.

Azelastine hydrochloride (Astelin) is a phthalazinone derivative with antihistaminergic activity.

Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

Flunisolide hemihydrate is a corticosteroid, an orally active Glucocorticoid receptor activator with anti-inflammatory effects. flunisolide hemihydrate induces apoptosis in eosinophils and can be used in asthma or rhinitis, inflammatory diseases. Can be used in studies related to asthma or rhinitis, inflammation.

SB705498 is a TRPV1 antagonist for hTRPV1. SB-705498 has been investigated for the treatment of Rhinitis, Chronic Cough, and Non-allergic Rhinitis.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

1. Prunetin (Prunusetin) significantly reduces serum levels of inflammatory cytokines and mortality in mice challenged with lipopolysaccharide. 2. Prunetin mediates anti-obesity/adipogenesis effects by suppressing obesity-related transcription through a feedback mechanism that regulates the expression of adiponectin, adipoR1, adipoR2, and AMPK. 3. Prunetin and biochanin A are potent reducers of NF-κB and ERK activation, zonula occludens 1 tyrosine phosphorylation, and metalloproteinase-mediated shedding activity, which may account for the barrier-improving ability of these isoflavones. 4. Prunetin significantly suppresses ATP-induced mucin secretion from cultured RTSE cells; Prunetin inhibits the production of MUC5AC mucin protein induced by EGF or PMA from NCI-H292 cells; Prunetin also inhibits the expression of MUC5AC mucin gene induced by EGF or PMA from NCI-H292 cells.

R112 is an ATP-competitive inhibitor of Syk kinase. Ki=6 nM，IC50=226 nM.

Thonzylamine (neohetramine) is an antihistamine and anticholinergic drug. It is available as combination products with Clofedanol or Phenylephrine for temporary relief of symptoms of common cold, hay fever (allergic rhinitis) or other upper respiratory allergies.

11(S)-HETE, an (S) enantiomer of 11(R)-HETE and a type of oxylipin, is non-enzymatically synthesized from arachidonic acid. Compared to its counterpart, 11(S)-HETE levels are found to be elevated in both isolated human plasma and serum, as well as in LPS-stimulated isolated human plasma. Notably, patients with allergic rhinitis exhibit a decrease in 11(S)-HETE levels in their serum following one year of double-mite subcutaneous immunotherapy (DM-SCIT), correlating with an enhanced quality of life, particularly in aspects related to rhinoconjunctivitis.

Mometasone furoate-d3 is a deuterated compound of Mometasone furoate. Mometasone furoate has a CAS number of 83919-23-7. Mometasone furoate is a pregnadienediol derivative ANTI-ALLERGIC AGENT and ANTI-INFLAMMATORY AGENT that is used in the management of ASTHMA and ALLERGIC RHINITIS. It is also used as a topical treatment for skin disorders.

Dihydro montelukast is a potential impurity found in commercial montelukast preparations. Montelukast (sodium salt) is a potent and selective cysteinyl leukotriene 1 (CysLT1) receptor antagonist. Formulations containing montelukast are used for the treatment of asthma as well as for the symptoms associated with allergic rhinitis.

TAS 205 is an inhibitor of hematopoietic prostaglandin D synthase (H-PGDS; IC50= 55.8 nM).1It is selective for H-PGDS over lipocalin-type PGDS (L-PGDS) at 100 μM, as well as over enzyme and receptor panels at 10 μM. TAS 205 inhibits production of prostaglandin D2induced by A23187 in KU812 human and RBL-2H3 rat basophils with IC50values of 78.3 and 181.3 nM, respectively. It inhibits ovalbumin-induced nasal lavage fluid eosinophil infiltration and late-phase nasal obstruction in an ovalbumin-sensitized guinea pig model of allergic rhinitis when administered at a dose of 30 mg/kg. 1.Aoyagi, H., Kajiwara, D., Tsunekuni, K., et al.Potential synergistic effects of novel hematopoietic prostaglandin D synthase inhibitor TAS-205 and different types of anti-allergic medicine on nasal obstruction in a Guinea pig model of experimental allergic rhinitisEur. J. Pharmacol.875173030(2020)

M 12325 is used in the production of furosemide; rhinitis and occupational asthma were observed in workers from a lasamide production line.

PF-03654764 is an orally active, potent, and selective histamine H3 receptor antagonist with Ki values of 1.2 nM for human H3 and 7.9 nM for rat H3. It is often co-administered with Fexofenadine for the treatment of allergic rhinitis.

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.

Brompheniramine ((±)-Brompheniramine) is a potent, orally active alkylamine class antihistamine and a selective antagonist of the histamine H1 receptor (Kd = 6.06 nM). It has applications in the research of allergic rhinitis and exhibits anticholinergic, antidepressant, and anesthetic properties. Brompheniramine blocks calcium channels, sodium channels, and hERG channels with IC50 values of 16.12 μM, 21.26 μM, and 0.90 μM, respectively [1] [2] [3] [4].

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].

SCH-79687 is a histamine antagonist selective for the H3 subtype. This H3 antagonist may play a role in allergic rhinitis.

Fluocortin butyl ester is a developed corticosteroid compound with no detectable systemic corticosteroid activity when used topically. It appears to be an effective, well-tolerated topical steroid suitable for studies of perennial rhinitis.

Dimethindene maleate (SU 6518) is a histamine H1 antagonist and can be used in studies about the treatment of hypersensitivity reactions, pruritus and rhinitis.

Chlorpheniramine maleate (NCI-C55265) is a histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma.

Fluticasone Propionate-d5 is a deuterated compound of Fluticasone Propionate. Fluticasone Propionate has a CAS number of 80474-14-2. Fluticasone propionate, derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.

HSR-609, a histamine H1 receptor antagonist, is used potentially for the treatment of allergic rhinitis.

Ambicromil is used for allergic rhinitis.

GSK-1004723 is a novel antagonist of histamine H(1) and H(3) receptor. It represents a potential novel therapy for allergic rhinitis.

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.