bronchial

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.

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.

Salbutamol (Albuterol) stimulates beta2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of ATP to cyclic-3', 5'-adenosine monophosphate (cAMP). Salbutamol Sulfate is the sulfate salt of the short-acting sympathomimetic agent albuterol, a 1:1 racemic mixture of (R)-albuterol and (S)-albuterol with bronchodilator activity. Increased cAMP concentrations relax the bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. To a lesser extent, Salbutamol stimulates beta1-adrenergic receptors, thereby increasing the force and rate of myocardial contraction.

L-Hyoscyamine sulfate (Levsin Sulfate) is the sulfate salt of a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. Hyoscyamine functions as a non-selective, competitive antagonist of muscarinic receptors, thereby inhibiting the parasympathetic activities of acetylcholine on the salivary, bronchial, and sweat glands, as well as the eye, heart, bladder, and gastrointestinal tract. These inhibitory effects cause a decrease in saliva, bronchial mucus, gastric juices, and sweat. Furthermore, its inhibitory action on smooth muscle prevents bladder contraction and decreases gastrointestinal motility.

Letosteine (Viscotiol) is an orally active, effective, and safe expectorant that can be used in the study of acute or chronic respiratory diseases, for example, bronchopulmonary disease. Letosteine dissolves bronchial mucus and reduces symptoms of respiratory inflammation and restores gas exchanges and natural defense mechanisms in the lung[1] [2] [3].

Cromoglicic acid prevents the release of inflammatory chemicals such as histamine from mast cells.

Parogrelil Free Base (NM-702 Free Base) is a selective phosphodiesterase 3 inhibitor with bronchodilatory and anti-inflammatory effects, inhibits leukotriene (LT)D(4) and histamine-induced constriction of isolated guinea pig tracheal strips, and can be used in the study of bronchial asthma.

Isoproterenol (Norisodrine) is a non-selective and orally active β-adrenoceptor agonist.Isoproterenol is a potent peripheral vasodilator and bronchodilator.Isoproterenol can be used in the study of bradycardia and bronchial asthma for the treatment of heart block, bradycardia.

Diphylline (Diprophylline) is a xanthine derivative. Diphylline exerts bronchodilator effects and to a lesser extent vasodilator and diuretic properties. Diphylline probably acts as a competitive inhibitor of phosphodiesterase which leads to an increase in intracellular cAMP. This results in relaxation of bronchial smooth muscle and other smooth muscles. Diphylline may also antagonize adenosinereceptors. Diphylline is used in the treatment of acute bronchial asthma, chronic bronchitis and emphysema.

Zileuton (A 64077) is a synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma.

Chlorin E6 (CE6) is a second-generation photosensitizer with antitumor activity when used in combination with irradiation. In a mouse model of implanted fibrosarcoma, Chlorin E6 (2.5-10 mg/kg, i.v., 50-200 J/cm2 irradiation) resulted in complete tumor disappearance after varying degrees of irradiation. Agents including Chlorin E6 were tested in a Phase I clinical study in patients with early superficial squamous cell carcinoma of bronchial origin with favorable results (40 mg/m2, IV, 100 J/cm2 laser irradiation). In a Phase II clinical trial in patients with early stage lung cancer, the same mode of administration resulted in a complete response in 82.9% of patients. Chlorin E6 has been investigated as a nanotechnology drug delivery tool.

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.

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.

Betahistine (Vasomotal) is a histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers. Betahistine dihydrochloride is an anti-vertigo drug. It is commonly prescribed for balance disorders or to alleviate vertigo symptoms associated with Ménière's disease.

Urodilatin, an analogue of ANF-(99-126), serves as a diuretic-natriuretic regulatory peptide with applications in the study of acute renal failure, congestive heart failure, and bronchial asthma, among other conditions [1].

Betahistine mesylate (Extovyl) is a histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.

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.

Bethanechol chloride (Carbamyl-β-methylcholine chloride) is a slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, heart rate changes, and bronchial spasm.

GGTI 2133, a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50= 38 nM), exhibits 140-fold selectivity towards GGTase I compared to farnesyltransferase (IC50= 5,400 nM). The compound effectively inhibits the geranylgeranylation of RAP1A (IC50= 10 µM) without affecting the farnesylation of H-Ras (IC50= >30 µM). Moreover, GGTI 2133 reduces the growth, migration, and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control levels, respectively. When administered intraperitoneally at 5 mg/kg per day, it prevents eosinophil infiltration into the airways in a mouse model of allergic bronchial asthma, although it does not reduce chemokine levels. Additionally, GGTI 2133 thwarts naloxone-induced contraction of ileum in rats experiencing morphine withdrawal syndrome and mitigates the severity of withdrawal symptoms in vivo (ED50= 0.076 mg/kg).

Theophylline-d6 is intended for use as an internal standard for the quantification of theophylline by GC- or LC-MS. Theophylline is an inhibitor of phosphodiesterase. It is also an adenosine A1 and A2 receptor antagonist. Theophylline induces relaxation of isolated cat bronchial smooth muscle segments precontracted with acetylcholine. It inhibits ovalbumin-induced increases in bronchoalveolar lavage fluid (BALF) eosinophil infiltration in an ovalbumin-sensitized mouse model of allergic asthma. Formulations containing theophylline have been used in the treatment of asthma and chronic obstructive pulmonary disease (COPD).

Pipoxolan (HCl) is an antispasmodic drug. In vivo, the drug inhibited the contractions of intestines caused by neostigmine, barium chloride or injection of acetylcholine. The drug possesses ganglioplegic action and inhibited the decrease in blood pressure caused by stimulation of the vagus nerve. The drug is marketed under tradename Rowapraxin worldwide for the treatment of spasms and colics in the gastrointestinal tract, gallbladder and urogenital area, bronchial spasms, spastic menstrual cramps. Recent studies have shown that pipoxalan has anticancer activity and inhibits proliferation of leukemia cells in animal models.

Faltan (Folpet),a widely used dicarboximide fungicide,induces tumors in the mouse gastrointestinal tract,primarily in the duodenum,and is also cytotoxic effect on human bronchial epithelial cells.

Piperilate, also known as Pipethanate, is a hetrazepine derivative PAF antagonist and anticholinergic mixture, commonly utilized in bronchial asthma research. This compound exhibits hypotensive properties and has been found to effectively counteract the toxic effects of organophosphates in mice [1] [2] [3].

CGP 45715A (irukostat) is a potent peptide-leukotriene antagonist used to treat respiratory diseases by antagonizing the bronchial constriction, mucus secretion, and inflammatory effects of these leukotrienes.

KAA-276 HCl is the salt form of KAA-276 free base, a novel potent and long-lasting histamine HI-receptor antagonist with less-topical irritation, and can be topically administered by inhalation for the treatment of bronchial asthma.

NP-1815-PX is a selective P2X4R antagonist with demonstrated anti-inflammatory effects and the capability to alleviate pain in chronic pain models. Additionally, it impedes contractions of guinea pig tracheal and bronchial smooth muscle (TSM and BSM)[1][2][3].

KAA-276 free base is a novel potent and long-lasting histamine HI-receptor antagonist with less-topical irritation, and can be topically administered by inhalation for the treatment of bronchial asthma.

Fevipiprant (NVP-QAW039) is a selective, potent, reversible competitive CRTh2 antagonist.

Folpet-d4 is a deuterated compound of Folpet. Folpet has a CAS number of 133-07-3. Folpet,a widely used dicarboximide fungicide,induces tumors in the mouse gastrointestinal tract,primarily in the duodenum,and is also cytotoxic effect on human bronchial epithelial cells.

Thunberginol C exhibits antimicrobial activity against oral bacteria. It shows antiallergic activity in the in vitro bioassay using the Schults-Dale reaction in sensitized guinea pig bronchial muscle.

FIZZ-1 (32-51) (mouse), a cysteine-rich secretory protein, is predominantly expressed in macrophages, bronchial epithelial, and type II alveolar epithelial cells (AEC) during allergic airway inflammation. Additionally, it exhibits an anti-apoptotic effect on lung fibroblasts, indicating its potential utility in researching allergic pneumonia [1] [2].

Histamine dihydrochloride (Ceplene) is dihydrochloride form of Histamine. Histamine is an organic nitrogen compound which is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.

Coumalic acid (Cumalic Acid) can be prepared from malic acid. It can be used in the industrial production of spices, flavorings, and cosmetics. It serves as a polymer component as well as an active molecular scaffold with anti-bronchial and malarial activity.

Propantheline bromide (Pro-Banthine) competitively antagonizes acetylcholine activity mediated by muscarinic receptors at neuroeffector sites on smooth muscle and exocrine gland cells. Propantheline Bromide is the bromide salt form of propantheline, a quaternary ammonium compound structurally related to belladonna alkaloids. An aspartic acid residue present in the N-terminal portion of the third transmembrane helix of the muscarinic receptor is believed to form an ionic bond with the tertiary or quaternary nitrogen of the antagonist. Antagonism leads to a reduction of exocrine glands secretions and to relax the bronchial muscle and reduce tone and motility of intestinal smooth muscle.

Arpenal HCl is a ganglionic blocking agent which may be useful in the treatment of bronchial asthma.

Pemirolast is an orally active antiallergic agent. Pemirolast attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides, that can be used for bronchial asthma and conjunctivitis research [1] - [5].

Tranilast Sodium has been used for the treatment of bronchial asthma. Tranilast is also used to autoimmune diseases, atopic and fibrotic pat.

Salbutamol-d9 is a deuterated compound of Salbutamol. Salbutamol has a CAS number of 18559-94-9. Albuterol stimulates beta2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of ATP to cyclic-3', 5'-adenosine monophosphate (cAMP). Albuterol Sulfate is the sulfate salt of the short-acting sympathomimetic agent albuterol, a 1:1 racemic mixture of (R)-albuterol and (S)-albuterol with bronchodilator activity. Increased cAMP concentrations relax the bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. To a lesser extent, albuterol stimulates beta1-adrenergic receptors, thereby increasing the force and rate of myocardial contraction.

PF-4348235 HCl (β2AR/M-receptor agonist-2 HCl) is a muscarinic M3 receptor antagonist (Ki: 0.73 nM) and β2 adrenergic receptor agonist (MABA, EC50: 3.7 nM). PF-4348235 HCl is also a bronchial BM213 acetate is a bronchodilator used to study cardiovascular and respiratory diseases such as chronic obstructive pulmonary disease (COPD).

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

RNF5 inhibitor inh-02, a potent E3 ubiquitin ligase RNF5/RMA1 inhibitor, demonstrates significant efficacy in rescuing F508del-CFTR with an EC50 of 2.2 uM in bronchial epithelial cells homozygous for the F508del mutation. This compound is valuable for cystic fibrosis research[1].

S-5751, a prostanoid DP (DP1) antagonist, is used potentially for the treatment of bronchial asthma.

Trans-Tranilast is an antiallergic drug developed by Kissei Pharmaceuticals. It was approved in 1982 for use in Japan and South Korea for bronchial asthma. Indications for keloid and hypertrophic scar were added in 1993. It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.

N-3-oxo-dodecanoyl-L-Homoserine lactone (3-oxo-C12-HSL), a quorum-sensing signaling molecule, is synthesized by P. aeruginosa and specific B. cepacia complex strains [1][2]. This regulatory mechanism facilitates bacterial gene expression modulation in response to cell density escalation. In 16HBE human bronchial epithelial cells, it triggers IL-8 production [3].

SRI-41315, a chemical compound, effectively addresses premature termination codons (PTCs) associated with cystic fibrosis in immortalized and primary human bronchial epithelial cells. It induces a prolonged pause at stop codons, resulting in the restoration of cystic fibrosis transmembrane conductance regulator (CFTR) expression and function. This compound achieves PTC suppression by reducing the abundance of the termination factor eRF1. Additionally, SRI-41315 synergistically enhances CFTR activity by potentiating aminoglycoside-mediated readthrough [1].

Desloratadine-d5 is a deuterated compound of Desloratadine. Desloratadine has a CAS number of 100643-71-8. Desloratadine 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.

Arpenal is a ganglionic blocking agent which may be useful in the treatment of bronchial asthma.

Ambroxol (NA-872) is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. It is the active ingredient of Mucosolvan, Lasolvan or Mucoangin. The substance is a mucoactive drug with several properties including secretolytic and secretomotoric actions that restore the physiological clearance mechanisms of the respiratory tract which play an important role in the body's natural defense mechanisms. It stimulates synthesis and release of surfactant by type II pneumocytes. Surfactants act as an anti-glue factor by reducing the adhesion of mucus to the bronchial wall, in improving its transport and in providing protection against infection and irritating agents.

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].

1,1-Diphenyl-4-(pyrrolidin-1-yl)but-2-yn-1-ol is an anticholinergic agent that has the potential for the research of bronchial asthma [1].