nasal

Quazolast (RHC 3988) is a potent mediator release inhibitor used as a control against ragweed antigenic nasal challenge and demonstrates superiority over placebo in preventing nasal congestion and nasal itching following such challenges.

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].

Cetylpyridinium chloride monohydrate (Hexadecylpyridinium chloride monohydrate) , a cationic quaternary ammonium compound, is used in certain classes of throat sprays, mouthwashes, lozenges, toothpaste, nasal sprays, and breath sprays. Cetylpyridinium chloride monohydrate has also been used as an ingredient in certain pesticides. It is an antiseptic with killing bacteria and other microorganisms. It can be potent in reducing gingivitis and preventing dental plaque. It may result in brown stains between the teeth and on the surface of teeth.

Sodium salicylate (2-Hydroxybenzoic acid sodium salt), a metabolite of acetylsalicylic acid, can inhibit NF-kB and reduce oxidative stress.

Mebhydrolin napadisylate (Incidal) is an antihistamine used to relieve allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis.

Synephrine (Oxedrine) is sympathetic alpha-adrenergic agonist used as a vasoconstrictor in circulatory failure, asthma, nasal congestion, and glaucoma.

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.

Xylometazoline hydrochloride (Xylometazoline HCl) is an α-adrenoceptor agonist usually used as nasal decongestant.

Tetrahydrozoline hydrochloride (Murine Plus) is an imidazoline derivative with alpha receptor agonist activity.

N-Nitrosodiethylamine (NDEA) is a potent hepatocarcinogenic dialkylnitrosoamine primarily found in water, tobacco smoke, cheddar cheese, cured and fried meals, and many alcoholic beverages. NDEA is responsible for changes in nuclear enzymes related to DNA repair replication and induces various tumors in all animal species, targeting mainly the liver, nasal cavity, trachea, lung, and esophagus.

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.

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.

2′-Deoxy-2′-fluoroguanosine is a nucleoside analog that potently inhibits influenza virus A and B strains(EC90 <0.35 μM). 2'-Deoxy-2'-fluoroguanosine is an inhibitor of influenza virus replication in the upper respiratory tract, improving fever and nasal inflammation.

Epimagnolin A is a lignan obtained from the flower buds of Magnolia fargesii, which is traditionally used in Asian medicine for treating headache and nasal congestion.

ARC 239 dihydrochloride is a selective α2B adrenoceptor antagonist with pKD values of 8.8, 6.7, and 6.4 at α2B, α2A, and α2D receptors respectively (pKD values are 8.8, 6.7, and 6.4 at α2B, α2A, and α2D receptors respectively).

Tetrahydrozoline (Tetryzoline), an alpha agonist, have an effect on the constriction of conjunctival blood vessels. This contributes to relieve the redness of the eye resulted from minor ocular irritants.

Tuaminoheptane is a sympathomimetic and vasoconstrictor that was once used as a nasal decongestant. It works by inhibiting and accelerating the release of norepinephrine, a mechanism that likely underpins its decongestant and stimulating effects. Unlike other norepinephrine-releasing agents such as phenethylamines, Tuaminoheptane's chemical structure lacks an aromatic ring. Additionally, it acts as a skin irritant and may cause contact dermatitis by inhibiting volume-regulated cation channels, which limits its utility as a decongestant.

14,15-Leukotriene D4 (14,15-LTD4) is a member of an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-lipoxygenases (15- and 12-LOs) on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. 14,15-LTD4 is classified as an eoxin (EXD4), because it is formed mostly by eosinophils. However, mast cells and nasal polyps can synthesize 14,15-LTD4 as well. Little is known about the physiological actions of 14,15-LTD4. It has weak contractile activity on both guinea pig ileum and pulmonary parenchyma in contrast to the effects of 5-LO-derived LTs. However, in an in vitro permeability assay, 14,15-LTD4 can increase vascular permeability of human endothelial cell monolayers, with similar potency to that of 5-LO-derived LTs, resulting in plasma leakage, a hallmark of inflammation.

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)

Clonazoline is a coronary vasodilator that is an imidazoline sympathomimetic, an alpha-adrenoreceptor agonist. It was used as a nasal decongestant and vasoconstrictor.

Pepsin is an endopeptidase that breaks down proteins into smaller peptides and amino acids that can be easily absorbed in the small intestine[1]. Pepsin is stable at pH ranges as high as pH 6. Above this pH, pepsin is rapidly irreversibly inactivated and elevation of pH of the reaction mixture to pH 8 results in complete inactivation of pepsin[2]. Pepsin has been posited to be a reliable biological marker of EER. An immunologic pepsin assay of combined sputum and saliva was determined to be 100% sensitive and 89% specific for detection of EER (based on pH-metry), and an enzymatic test of nasal lavage fluid (100% sensitivity and 92.5% specificity) demonstrated an increased incidence of EER in patients with chronic rhinosinusitis[3]. Cultured hypopharyngeal epithelial (FaDu) cells were exposed to human pepsin (0.1 mg mL) at pH 7.4 for either 1 hour or 12 hours at 37°C and both mitochondria and Golgi complexes were clearly damaged. This finding reveals a novel mechanism by which pepsin could cause cell damage, potentially even in nonacidic refluxate[4].

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.

(-)-Fargesol is a nartural product from the flowers buds of Magnolia fargesii,the dried flower buds of M. fargesii, has been used as therapy for nasal empyema and headache.

Tuaminoheptane was originally developed as a nasal decongestant and belongs to the class of sympathomimetics and vasoconstrictors. It exhibits decongestant and stimulating effects by inhibiting and releasing norepinephrine. Unlike phenethylamine-based norepinephrine releasers, Tuaminoheptane has a unique chemical structure. Additionally, it may cause contact dermatitis due to its potential to irritate the skin by inhibiting volume-regulated anion channels, which limits its effectiveness as a decongestant.