rhinitis

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.

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

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

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

Fluticasone furoate (Avamys) is a synthetic trifluorinated corticosteroid derived from fluticasone with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflammatory, anti-asthmatic activity, and low systemic exposure. Fluticasone furoate can be used as a nasal spray for studies about allergic rhinitis treatment.

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.

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

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.

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.

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.

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.

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.

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

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.

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.

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].

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.

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.

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

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

Loratadine (SCH 29851) is a second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.

Fexofenadine hydrochloride (Terfenidine carboxylate hydrochloride) is a second generation antihistamine that is used for the treatment of allergic rhinitis, angioedema and chronic urticaria.

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.