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Related Concept Videos

Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

Direct-Acting Cholinergic Agonists: Pharmacokinetics

1.0K
Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
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Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

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Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...
817
Direct-Acting Cholinergic Agonists: Therapeutic Uses01:11

Direct-Acting Cholinergic Agonists: Therapeutic Uses

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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...
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Direct-Acting Cholinergic Agonists: Pharmacological Actions00:59

Direct-Acting Cholinergic Agonists: Pharmacological Actions

1.1K
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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Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

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Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
503
Indirect-Acting Cholinergic Agonists: Pharmacological Actions01:30

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

588
Indirect-acting cholinergic agonists, also known as anticholinesterases, exert their pharmacological effects by enhancing cholinergic transmission in various body parts, including the neuromuscular junction, autonomic cholinergic synapses, and the brain.
At the neuromuscular junction, these agents work by inhibiting the breakdown of acetylcholine, allowing it to remain bound to the receptor and bind to nearby receptors. This process leads to repetitive firing of the endplate, causing muscle...
588

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Related Experiment Video

Updated: May 20, 2025

Probing Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices via Laser Flash Photolysis of Photoactivatable Nicotine
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Light-Activated Pharmacological Tools for Exploring the Cholinergic System.

Alessio Colleoni1,2, Giulia Galli1, Clelia Dallanoce1

  • 1Section of Medicinal Chemistry "Pietro Pratesi", Department of Pharmaceutical Sciences, University of Milan, Milan, Italy.

Medicinal Research Reviews
|March 24, 2025
PubMed
Summary
This summary is machine-generated.

Light-activated drugs offer precise control over cholinergic signaling, overcoming limitations of traditional medications. This photopharmacology approach enhances therapeutic potential for neurological and inflammatory conditions.

Keywords:
muscarinic acetylcholine receptorsnicotinic acetylcholine receptorsphotopharmacologyphotoswitchuncaging

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Related Experiment Videos

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Biochemistry

Background:

  • Cholinergic transmission is vital for central and peripheral nervous system functions, including learning, memory, and inflammation.
  • Conventional cholinergic drugs lack selectivity and temporal precision, causing side effects and limiting treatment effectiveness.
  • Photopharmacology utilizes light-activated compounds for precise spatiotemporal control over biological processes.

Purpose of the Study:

  • To review the development and application of light-activated cholinergic modulators.
  • To explore their use in understanding cholinergic signaling in health and disease.
  • To highlight their potential for novel phototherapeutic strategies.

Main Methods:

  • Review of literature on photocleavable and photoswitchable ligands targeting cholinergic systems.
  • Analysis of studies employing light to modulate muscarinic, nicotinic, and cholinesterase activities.
  • Examination of applications in physiological and pathological research.

Main Results:

  • Development of diverse light-activated compounds for cholinergic modulation.
  • Demonstration of precise spatiotemporal control over cholinergic signaling pathways.
  • Evidence for utility in dissecting cholinergic roles in various biological contexts.

Conclusions:

  • Photopharmacology offers a powerful strategy to overcome limitations of conventional cholinergic drugs.
  • Light-activated cholinergic agents provide unprecedented tools for research and potential therapeutics.
  • This approach promises innovative treatments for neurological and inflammatory disorders.