Related Experiment Video
Updated: Jul 7, 2026
04:50
Direct Tracheal Instillation of Solutes into Mouse Lung
Published on: August 29, 2010
New 8-substituted xanthiene derivatives as potent bronchodilators
Barkin Berk1, Hülya Akgün, Kevser Erol
1Yeditepe University, Faculty of Pharmacy, 26 Ağustos Yerleşimi, 34755, Kayişdaği, Istanbul, Turkey.
Farmaco (Societa Chimica Italiana : 1989)
|October 26, 2005
Summary
New purine derivatives were synthesized and tested for bronchodilator and anti-inflammatory effects. Compound 11 selectively antagonized adenosine A2B receptors, showing potential as an anti-inflammatory agent for asthma treatment.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Drug Discovery
Background:
- Theophylline is a bronchodilator, but its efficacy is limited.
- Adenosine receptors play a role in inflammatory and respiratory diseases.
- Novel purine derivatives offer potential therapeutic avenues.
Purpose of the Study:
- To synthesize and characterize novel 1,3-dimethyl-3,7-dihydropurine-2,6-dione derivatives.
- To evaluate the bronchodilator and spasmolytic activities of these compounds.
- To investigate their potential as adenosine receptor antagonists.
Main Methods:
- Synthesis and structural determination of 13 purine derivatives.
- In vitro assessment of bronchodilator activity using guinea-pig tracheal strips.
- Radioligand binding and cAMP functional assays to evaluate adenosine receptor antagonism.
Main Results:
- Compounds showed limited bronchodilator activity against acetylcholine.
- Several compounds inhibited histamine-induced contractions, with compounds 7, 11, and 12 being most effective.
- Compound 11 demonstrated significant antagonism at adenosine A2A and A2B receptors, with selectivity over A1 and A3 subtypes.
- Compound 11 was also the most potent inhibitor of NECA-induced cAMP accumulation via the A2B receptor.
Conclusions:
- The synthesized purine derivatives act as selective adenosine receptor antagonists, particularly for the A2B subtype.
- These compounds show promise as anti-inflammatory agents for conditions like asthma, rather than direct bronchodilators.
Related Concept Videos
01:11Direct-Acting Cholinergic Agonists: Therapeutic Uses
Direct-acting cholinergic agonists have many therapeutic uses in various medical fields. Choline esters, including acetylcholine, have limited clinical utility due to their non-selectivity and short duration of action. Still, acetylcholine and carbachol are applied topically during ophthalmologic surgery to induce miosis. Pilocarpine, a muscarinic and ganglionic stimulator, effectively treats open-angle glaucoma and alleviates xerostomia and dry mouth caused by radiotherapy or Sjögren syndrome.
01:17Drugs Used in Lower Respiratory Disorders: Overview
Lower respiratory tract disorders present challenges that often require skilled and nuanced approaches for effective management. Common ailments, such as asthma and chronic obstructive pulmonary disease (COPD), have prompted the development of intricate treatment strategies involving bronchodilators and anti-inflammatory drugs, each tailored to ease breathing and revitalize the lungs.
Bronchodilators, the first step of respiration enhancement, come in various forms, each with its own mechanism...
Bronchodilators, the first step of respiration enhancement, come in various forms, each with its own mechanism...
01:25Antiasthma Drugs: β2-Adrenoceptor Agonists
Bronchodilators are critical in managing asthma, a chronic respiratory condition characterized by airway constriction due to inflammation and hyper-reactivity. Specifically, bronchodilators ease this constriction by relaxing the bronchial muscles, facilitating easier breathing.
One class of bronchodilators includes β2-adrenoceptor agonists. These agents target the β2-adrenoceptors located on bronchial smooth muscle cells. By stimulating these receptors, β2-agonists induce relaxation in these...
One class of bronchodilators includes β2-adrenoceptor agonists. These agents target the β2-adrenoceptors located on bronchial smooth muscle cells. By stimulating these receptors, β2-agonists induce relaxation in these...
01:24Antiasthma Drugs: Methylxanthines
Theophylline, a member of the methylxanthine class of bronchodilators, has long been used in asthma management. While its exact mechanism of action is not fully understood, it is believed to have multiple effects on various cellular processes.
Theophylline is thought to inhibit phosphodiesterase enzymes, increasing intracellular levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). This rise in cAMP and cGMP concentrations stimulates cardiac function,...
Theophylline is thought to inhibit phosphodiesterase enzymes, increasing intracellular levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). This rise in cAMP and cGMP concentrations stimulates cardiac function,...
01:19Antiasthma Drugs: Leukotriene Modifiers
Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:
Leukotriene modifiers work through two distinct mechanisms:
01:20Antiasthma Drugs: Muscarinic Receptor Antagonists
Muscarinic receptor antagonists, also known as antimuscarinic agents, are a class of bronchodilators used to treat asthma, although they are more commonly used to treat COPD. They work by inhibiting the action of acetylcholine (ACh), a neurotransmitter, on muscarinic receptors found in the airways.
Antimuscarinic agents compete with ACh for the same binding site on the muscarinic receptors. By binding to these receptors, they inhibit the downstream effects of ACh and block the parasympathetic...
Antimuscarinic agents compete with ACh for the same binding site on the muscarinic receptors. By binding to these receptors, they inhibit the downstream effects of ACh and block the parasympathetic...