hyperresponsiveness

BEC hydrochloride (BEC HCl) is a competitive arginase inhibitor, which bind slowly. Ki of BEC HCl is 0.31 μM (pH7.5) for Arginase II, and is 0.4-0.6 μM for rat Arginase I.

RS-601 is a potent dual leukotriene D4 thromboxane A2 inhibitor that inhibits antigen-induced airway hyperresponsiveness (AHR) and shows asthmatic effects in a guinea pig model of asthma.

Pirodomast is a thromboxane A (TXA2) synthase inhibitor. Pirodomast inhibits leukotriene (LT) D4, C4, E4 formation and thromboxane B2 (TXB2) activity, but is weakly or ineffectively antagonistic to guinea pig bronchospasm induced by histamine, methacholine, serotonin, LTC4, or platelet-activating factor. Pirodomast is a potential antiallergic compound. Pirodomast had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is a potential antiallergic compound that inhibits the protein hydrolyzing activity of trypsin in vitro, prevents antigen-induced immediate and late asthmatic responses in allergic sheep in vivo, and inhibits antigen-induced airway hyperresponsiveness to histamine and carbachol in allergic sheep.

picumeterol FA is a potent and selective β2-adrenergic receptor agonist. In in vitro and in vivo tests, picumeterol FA produces long-lasting airway smooth muscle relaxation. picumeterol FA is a pure R-enantiomer and can be used to improve lung function and reduce airway hyperresponsiveness in patients with asthma.

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.

2-Methylbutyrylcarnitine (chloride) acts as a gut microbial metabolite that targets integrin α2β1 on platelets, facilitating the activation of cytosolic phospholipase A2 (cPLA2) and enhancing platelet hyperresponsiveness. This compound further augments platelet hyperreactivity and promotes thrombus formation in mice. It is also characterized as a branched-chain acylcarnitine.

Acetyl tetrapeptide-15 Acetate (Skinasensyl Acetate), a synthetic peptide used in cosmetic products for sensitive skin, is an endomorphin-2 derivative that extends the range of neuronal excitability thresholds in the μ-opioid receptor via an endorphin-like pathway, and can be used to study inflammatory and neuropathic pain produced by skin hyperreactivity. Inflammatory and neuropathic pain produced by skin hyperresponsiveness.

APC 366 is a selective inhibitor of mast cell tryptase with a Ki of 7.1 μM. It inhibits antigen-induced early asthmatic response (EAR), late asthmatic response (LAR), and bronchial hyperresponsiveness (BHR) in a sheep model of allergic asthma [1] [2].

ONO-8809 is a thromboxane A2 receptor antagonist. ONO-8809 inhibited the LTC4-induced airway hyperresponsiveness to histamine in a dose-dependent manner. Macrophage accumulation and matrix metalloproteinase-9 (MMP-9) activity in the stroke-negative area i

Sul-121 has anti-oxidative capacity. In experimental chronic obstructive pulmonary disease (COPD) models, Sul-121 HCl inhibits airway inflammation and hyperresponsiveness (AHR) prospectively through inhibition of oxidative stress.

Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered topically or subcutaneously at doses of 0.01-1% or 1 mg/kg, respectively.3It increases maximal lung pressure volume curves in fetal sheep when administered to pregnant ewes at 0.75 gestation at doses of 80 and 170 μg/kg.1Betamethasone 21-phosphate increases body weight, impairs learning and memory, increases anxiolytic behavior, and reduces hippocampal neurogenesis in CD-1 mice but reduces body weight and increases neurogenesis with no effect on anxiety in high-anxiety DBA/2 mice when administered at a dose of approximately 25 mg/kg per day in the drinking water for seven weeks.4Formulations containing betamethasone 12-phosphate and betamethasone acetate have been used in the treatment of severe allergic conditions and a variety of immune-related conditions. 1.Loehle, M., Schwab, M., Kadner, S., et al.Dose-response effects of betamethasone on maturation of the fetal sheep lungAm. J. Obstet. Gynecol.202(2)186.e181-186.e187(2010) 2.Leusink-Muis, A., Ten Broeke, R., Folkerts, G., et al.Betamethasone prevents virus-induced airway inflammation but not airway hyperresponsiveness in guinea pigsClin. Exp. Allergy29(Suppl. 2)82-85(1999) 3.Tsuji, F., Sawa, K., Kato, M., et al.The effects of betamethasone derivatives on endotoxin-induced uveitis in ratExp. Eye Res.64(1)31-36(1997) 4.Aiello, R., Crupi, R., Leo, A., et al.Long-term betamethasone 21-phosphate disodium treatment has distinct effects in CD1 and DBA/2 mice on animal behavior accompanied by opposite effects on neurogenesisBehav. Brain Res.278155-166(2015)

Methacholine bromide (Acetyl-β-methylcholine bromide) is a potent muscarinic-3 (M3) agonist that specifically acts on acetylcholine receptors located on smooth muscle, inducing bronchoconstriction and narrowing of the airways. Its high sensitivity in identifying bronchial hyperresponsiveness (BHR), a hallmark of asthma, makes it useful in the assessment of airway hyperresponsiveness (AHR) as a diagnostic tool for individuals exhibiting asthma-like symptoms with normal resting expiratory flow rates [1] [2] [3] [4].

JT002 is an orally active NLRP3 inflammasome inhibitor that decreases the production of NLRP3-dependent proinflammatory cytokines (such as IL-1β, IL-1α, IL-18) and pyroptosis, as well as inhibits the formation of the NLRP3 inflammasome complex. Additionally, JT002 mitigates airway hyperresponsiveness and airway neutrophilia in mice [1].

HYDAMTIQ, a PARP-1 2 inhibitor (IC 50 : 29-38 nM), exhibits a range of pharmacological effects including anticancer, anti-inflammatory, and ischemic protective properties. It effectively reduces pulmonary PARP activity and alleviates symptoms such as allergen-induced cough and dyspnea while also diminishing bronchial hyperresponsiveness to methacholine. Moreover, HYDAMTIQ shows potent tumor suppressor activity in various cancers such as ovarian, breast, prostate, pancreatic, and glioblastoma multiforme. Demonstrating in vivo efficacy, HYDAMTIQ has been tested in animal models for conditions like cerebral ischemia, asthma, and cancer [1].

Ayanin has vasorelaxant activity, it also may have the potential for use in treating allergic asthma.The IC(50) value of Ayanin (quercetin-3,7,4'-O-trimethylether) is 2.2microM for inhibiting interleukin (IL)-4 production from purified basophils.

Quercetin 3-O-methyl ether is a potent phosphodiesterase (PDE)3 4 inhibitor, it has potential for treating asthma against ovalbumin-induced airway hyperresponsiveness.