airway smooth muscle

Theophylline (1,3-Dimethylxanthine) is a methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac, and central nervous system stimulant activities. It inhibits the 3', 5'-cyclic nucleotide phosphodiesterase that degrades cyclic AMP, thus potentiating the actions of agents that act through adenylyl cyclases and cyclic AMP.

Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.

SKF96067 is a reversible gastric H+/K+-ATPase inhibitor that can induce relaxation of human airway smooth muscle in vitro.

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.

PD-102807 is a selective and competitive M4 muscarinic receptor antagonist (IC50 = 90.7 nM), with IC50 values of 950–7412 nM for M1, M2, M3, and M5 receptors, and can be used for Parkinson's disease research, as well as to inhibit airway smooth muscle (ASM) contraction.

Ethacrynic acid, a diuretic, functions as an inhibitor of L-type voltage-dependent and store-operated calcium channels, facilitating the relaxation of airway smooth muscle (ASM) cells. It exhibits anti-inflammatory effects, notably reducing retinoid-induced ear edema in mice, and inhibits glutathione S-transferases (GSTs), making it a potent suppressor of the NF-kB signaling pathway. Additionally, ethacrynic acid modulates leukotriene formation. A variant, Ethacrynic acid D5, is distinguished by its deuterium labeling.

PPADS tetrasodiuma is a potent P2X receptor antagonist and inhibitor of the inverse mode of Na/Ca²⁺ exchange in guinea pig airway smooth muscle and is neuroprotective against glutamate/NMDA toxicity.PPADS tetrasodiuma inhibits P2X1, P2X-2, P2X-3, and P2X- 5. 5.

(S)-Albuterol functions as a muscarinic receptor and phospholipase C activator, enhancing the intracellular free calcium concentration in airway smooth muscle cells.

RCD405 is a bronchodilator that exerts a relaxing effect by directly acting on human airway smooth muscle (hASM), with an EC50 value of 12 μM for histamine-induced contraction and 45.71 μM for carbachol-induced contraction. It inhibits cholinergic and histaminergic tension and reduces contractions induced by electrical field stimulation (EFS). RCD405 shows potential for research in asthma and chronic obstructive pulmonary disease (COPD).

Vilanterol (GW642444) acetate is a long-acting β2-AR agonist. The pEC50 values for vilanterol acetate are 9.4 for β2-AR, 6.4 for β1-AR, and 6.1 for β3-AR, indicating its selectivity in activating airway β2-AR receptors. This activation elevates cAMP levels, resulting in the relaxation of bronchial smooth muscle. Vilanterol acetate can be used in asthma-related research.

Indimilast is used to inhibit phosphodiesterase IV that regulates lung inflammation and causes bronchiectasis by increasing intracellular cyclic adenosine 3', 5'-monophosphate in airway smooth muscle and inflammatory cells. Potential to treat chronic obst

Urotensin II-related peptide acetate are endogenous ligands of the orphan G-protein-coupled receptor GPR14, now known as UT. Urotensin II and URP exert a wide spectrum of biological effects on peripheral tissues including the cardiovascular system, airway smooth muscle, kidneys, and endocrine glands, while central administration elicits complex behavioral and cardiovascular responses, highlighting their physiological and pharmacological significance.

Trifolirhizin exerts varying degrees of inhibition on tyrosinase-dependent melanin biosynthesis, and therefore, are candidates as skin-whitening agents.Trifolirhizin possesses potential anti-inflammatory and anti-cancer activities.Trifolirhizin shows in vitro inhibitory effects on the growth of human A2780 ovarian and H23 lung cancer cells. Trifolirhizin inhibits acetylcholine mediated airway smooth muscle (ASM) contraction or directly relaxes pre-contracted ASM independent of β 2 -adrenoceptors.

Clorprenaline is a β-adrenergic receptor agonist that activates adenylate cyclase and PKA and upregulates cAMP, leading to relaxation of bronchial smooth muscle cells, dilation of the airway, and improvement of airflow. Clorprenaline inhibits the release of mediators, such as histamine and leukotrienes, from mast cells, further promoting its anti-inflammatory properties.

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].

Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor that targets PDE3 to relax airway smooth muscle and is used in asthma and chronic obstructive pulmonary disease (COPD) research. It also functions as an adenosine receptor antagonist, histone deacetylase (HDAC) activator, and exhibits anti-inflammatory activity by increasing IL-10 levels and inhibiting NF-κB nuclear import, while inducing apoptosis [1] [2] [3] [4] [5].

Tiotropium Bromide hydrate (BA-679 BR hydrate) is a potent anticholinergic and bronchodilator, serving as a muscarinic receptor antagonist, specifically targeting mAChR. It is developed for treating chronic obstructive airways disease (COPD), demonstrating novel and long-lasting effects. Binding studies with [3H]tiotropium bromide in human lung reveal its high potency and equivalent affinity for M1-, M2-, and M3-receptors, making it roughly 10 times more effective than ipratropium bromide. It notably inhibits cholinergic nerve-induced contraction of both guinea-pig and human airways more potently than atropine or ipratropium bromide, albeit with a slower onset. Tiotropium bromide uniquely presents slow dissociation from M3-receptors on airway smooth muscle and rapid dissociation from M2 autoreceptors on cholinergic nerve terminals. As a quaternary ammonium derivative, it shows high affinity and special kinetic selectivity towards muscarinic receptors across M1-, M2-, and M3-subtypes, due to its slower dissociation from M1- and M3-receptors compared to M2-receptors.

Picumeterol(GR 114297A) is a potent and selective β2 adrenergic receptor agonist. In vitro and in vivo trials, Picumeterol produced long-lasting airway smooth muscle relaxation. Picumeterol is a pure R enantiomer that can be used to improve lung function and reduce airway hyperreactivity in patients with asthma.

DFPQ is a powerful and selective β-arrestin-biased negative allosteric modulator(NAM) targeting the β2-adrenergic receptor. It specifically inhibits the interaction of β-arrestin with β2AR without altering β-agonist-induced cAMP production. Additionally, DFPQ reduces functional desensitization of the β2AR in airway smooth muscle, enhancing β-agonists' capacity to maintain bronchorelaxation and curbing cell migration during prolonged β-agonist treatment.

Trifolirhizin (Standard) is a reference standard for research and analysis in studies involving Trifolirhizin. Trifolirhizin exerts varying degrees of inhibition on tyrosinase-dependent melanin biosynthesis, and therefore, are candidates as skin-whitening agents.Trifolirhizin possesses potential anti-inflammatory and anti-cancer activities.Trifolirhizin shows in vitro inhibitory effects on the growth of human A2780 ovarian and H23 lung cancer cells. Trifolirhizin inhibits acetylcholine mediated airway smooth muscle (ASM) contraction or directly relaxes pre-contracted ASM independent of β 2 -adrenoceptors.