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Related Concept Videos

Antiasthma Drugs: Muscarinic Receptor Antagonists01:20

Antiasthma Drugs: Muscarinic Receptor Antagonists

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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...
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Skeletal Muscle Relaxants: Therapeutic Uses01:31

Skeletal Muscle Relaxants: Therapeutic Uses

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Skeletal muscle relaxants are used to relax muscle tone and alleviate painful muscle contractions. However, the choice of skeletal muscle relaxants depends on the duration of the surgical procedure in order to minimize potential side effects. Skeletal muscle relaxants like neuromuscular blocking agents [NMBAs] are commonly employed as adjuvants alongside general anesthetics in clinical settings. NMBAs are also used to maintain controlled ventilation during surgery of the larynx or pharynx...
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Antiasthma Drugs: β2-Adrenoceptor Agonists01:25

Antiasthma Drugs: β2-Adrenoceptor Agonists

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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...
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Drugs Used in Lower Respiratory Disorders: Overview01:17

Drugs Used in Lower Respiratory Disorders: Overview

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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...
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Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacological Actions01:27

Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacological Actions

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Nondepolarizing neuromuscular blockers prevent the membrane depolarization of muscle cells and inhibit muscle contraction. These are usually administered with anesthetics to achieve complete muscle relaxation. Upon administration, these drugs first block the small, rapidly contracting muscles of the face and hands, followed by the larger muscles of the trunk and the intercostal muscles. The diaphragm is the last muscle to be affected.
Although all competitive neuromuscular blockers are designed...
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Direct-Acting Cholinergic Agonists: Pharmacological Actions00:59

Direct-Acting Cholinergic Agonists: Pharmacological Actions

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Direct-acting cholinergic agonists exert their pharmacological actions by mimicking the effects of acetylcholine on postsynaptic muscarinic receptors to generate parasympathetic responses. These agents elicit a range of physiological responses, including cardiovascular effects. For example, activation of muscarinic receptors induces bradycardia, decreased cardiac output, reduced peripheral resistance, and consequent hypotension. In the eye, stimulation of M3 receptors leads to smooth muscle...
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Related Experiment Video

Updated: Aug 9, 2025

In vitro Measurements of Tracheal Constriction Using Mice
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Design of Multitarget Inhibitors as Tracheal Smooth Muscle Relaxants.

Neela M Bhatia1, Manish S Bhatia2, Sibaprasad K Mohanty2

  • 1Department of Pharmaceutical Quality Assurance, BharatiVidyapeeth College of Pharmacy, Kolhapur, India.

Current Protein & Peptide Science
|February 24, 2023
PubMed
Summary
This summary is machine-generated.

New non-steroidal N-heteroarylamides show promise for asthma treatment by relaxing tracheal smooth muscles. These compounds target multiple pathways, offering an alternative to steroidal therapies with potential adverse effects.

Keywords:
AsthmaLTB4Tracheal smooth muscle relaxantscombinatorial synthesisinhaled corticosteroids (ICS)polyfunctional N-heteroarylamides

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Computational Chemistry

Background:

  • Steroidal therapies for asthma present complications and side effects.
  • There is a need for non-steroidal compounds that target multiple pathways in asthma.
  • Polyfunctional N-heteroarylamides are explored as potential non-steroidal asthma therapeutics.

Purpose of the Study:

  • To design and synthesize novel polyfunctional N-heteroarylamides.
  • To evaluate the tracheal smooth muscle relaxant effects of these compounds.
  • To investigate their potential as non-steroidal asthma treatments.

Main Methods:

  • Virtual screening and molecular docking against targets like FLAP, LTB4, and H1 receptor.
  • Combinatorial synthesis of a 5x5 mini-library of N-heteroarylamides.
  • In vitro evaluation of tracheal smooth muscle relaxation on isolated goat trachea.

Main Results:

  • Synthesized N-heteroarylamides demonstrated significant tracheal smooth muscle relaxant activity.
  • Activity was observed against both histamine and LTB4-induced contractions.
  • Structure-activity relationships were established based on screening results.

Conclusions:

  • The synthesized polyfunctional N-heteroarylamides possess tracheal smooth muscle relaxant properties.
  • Virtual screening predictions correlated well with observed biological activities.
  • These compounds represent a promising class of non-steroidal agents for asthma management.