bronchoconstriction

Atracurium besylate (51W89) is a non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.

Gemilukast (ONO-6950) is an orally active and potent dual inhibitor of cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2), inhibits LTC 4-induced bronchoconstriction, and is inhibitory to human CysLT1 and CysLT2, and may be used in the treatment of asthma.

FPL 55712 is a leukotriene receptor and SRS-A antagonist that inhibits bronchoconstriction and can be used in studies of asthma and coronary artery thrombosis.

Leukotriene C4 (LTC4) is an arachidonate lipid mediator that regulates leukocyte recruitment and function at sites of inflammation.Leukotriene C4 is a mediator of bronchoconstriction, mucus hypersecretion, and eosinophilia, and has a mediating role in urticaria.

Pipoxizine has an antagonistic effect on histamine-induced bronchoconstriction and may be used in the study of asthma disease.

Laprafylline is a xanthine compound with inhibitory effects on bronchoconstriction in vivo and antitumor activity.Laprafylline acts as a competitive serotonergic antagonist at low concentrations, and inhibits constriction induced by hist at high difficulties.

lodoxamide ethyl is a new orally active anti-allergic compound for the prevention of antigen-induced bronchoconstriction and blockage of skin allergic reactions.

ZD-2138 is a potent and selective specific inhibitor of 5-lipoxygenase (5-LOX) that inhibits allergen-induced pulmonary bronchoconstriction and reduces neurally-induced fast-acting kallikrein-ergic constriction of isolated airways in guinea pigs.ZD-2138 can be used for the treatment of asthma disease.

Doxylamine Succinate is a pyridine derivate histamine H1 antagonist with pronounced sedative properties. Doxylamine succinate (Decapryn) competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of the gastrointestinal smooth muscle, caused by actions of histamine on bronchial and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes.

Methacholine Chloride (Acetyl-β-methylcholine chloride) is a quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma.

Desloratadine (Sch34117) is a long-acting piperidine derivate with selective H1 antihistaminergic and non-sedating properties. Desloratadine diminishes the typical histaminergic effects on H1-receptors in bronchial smooth muscle, capillaries and gastrointestinal smooth muscle, including vasodilation, bronchoconstriction, increased vascular permeability, pain, itching and spasmodic contractions of gastrointestinal smooth muscle. Desloratadine is used to provide symptomatic relieve of allergic symptoms.

MK-571 sodium (L-660711 sodium salt) is a selective, orally active antagonist of the CysLT1 receptor. MK-571 sodium is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics, and their conjugates. MK-571 sodium can inhibit the synthesis of K-4′-O-GlcA (19.7 μM). MK571 dose-dependently inhibits the intracellular biosynthesis of all flavonol sulphates and glucuronides by Caco-2 cells. MK-571 sodium significantly inhibits phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-4′-O-glucuronide was competitively inhibited. In addition to inhibiting MRP2, MK571 is a potent inhibitor of enterocyte phase-2 conjugation.

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

TAK-661 is an inhibitor of eosinophil chemotaxis (eosinophil chemotaxis) that significantly alleviates late-phase bronchoconstriction while inhibiting the proliferation of eosinophils in bronchoalveolar lavage (BAL) and their infiltration into the airway walls.

TPI-1020 is a novel anti-inflammatory corticosteroid and nitric oxide (NO) donor derived from budesonide. It exhibits a concentration-dependent bronchodilatory effect mediated by released NO through a cGMP-dependent pathway. Studies suggest that TPI-1020 combines corticosteroid activity with NO release, potentially benefiting the treatment of acute bronchoconstriction events in asthma and allowing for a reduced dose of inhaled beta(2)-adrenoceptor agonists.

SR2640 is a potent and highly selective LTD4 LTE4 antagonist, specifically inhibiting LTD4-induced contractions in guinea pig ileum and tracheal smooth muscle in a concentration-dependent manner, without affecting histamine-induced contractions. It blocks the binding of 0.4 nM [3H]LTD4 to guinea pig lung membrane receptors with an IC50 of 23 nM. SR2640 also causes a parallel rightward shift in the dose-response curve for LTD4-induced bronchoconstriction in guinea pigs when administered intravenously, with the degree of shift correlating positively with its dosage. SR2640 is applicable for asthma research.

MIDD0301 (GL-II-93) sodium is an orally active inhibitor of γ-aminobutyric acid type A receptors (GABAAR) and an anti-asthmatic agent. It shows bio- and immunotoxicological safety in mice without affecting circulating lymphocyte, monocyte, and granulocyte counts. MIDD0301 sodium demonstrates no significant adverse immune responses under repeated dosing and is more favorable than Prednisone. It relaxes histamine-contracted tracheal smooth muscle in guinea pigs and humans, making it a valuable candidate for research in bronchoconstriction-related diseases.

CDP-840 (GR259653X) is a potent, selective, and orally active phosphodiesterase IV (PDE IV) inhibitor that specifically inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys [1].

Ablukast (Ro 23-3544) is a leukotriene receptor antagonist that functions as an anti-asthmatic.

BI-L 239 is an inhibition of 5-lipoxygenase products that cause bronchoconstriction.

Mequitamium iodide is a platelet activating factor (PAF) inhibitor. Mequitamium inhibits PAF-acether induced platelet aggregation and bronchoconstriction. Mequitamium is capable of inhibiting platelet-mediated effects of PAF by interfering with secondary

16,16-dimethyl Prostaglandin E1 is a PGE1 (T1626) analog that induces bronchoconstriction and vascular smooth muscle contraction and inhibits indomethacin-induced cell elongation.

11-deoxy Prostaglandin E1 is a prostaglandin E1 analogue that has bronchodilator activity and can inhibit histamine-induced bronchoconstriction and cause relaxation of tracheal strips in isolated guinea pigs.

Leukotriene C4 (LTC4) is the parent cysteinyl-leukotriene produced by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. LTC4 is produced by neutrophils, macrophages, and mast cells, and by transcellular metabolism in platelets. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute allergic hypersensitivity. The concentration of LTC4 required to produce marked contractions of lung parenchymal strips and isolated tracheal rings is about 1 nM. LTC4 methyl ester is a more lipid soluble form of LTC4. The biological activity of LTC4 methyl ester has not been reported.