Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Indirect-Acting Cholinergic Agonists: Mechanism of Action01:18

Indirect-Acting Cholinergic Agonists: Mechanism of Action

1.5K
Indirect-acting cholinergic agonists work by interacting with an enzyme called acetylcholinesterase (AChE) in the synaptic cleft. They can be reversible or irreversible inhibitors and have different effects on the enzyme.
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex,...
1.5K
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

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

515
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...
515
Anticholinesterase Agents: Poisoning and Treatment01:26

Anticholinesterase Agents: Poisoning and Treatment

779
Anticholinesterases, also known as cholinesterase inhibitors, work by blocking the breakdown of acetylcholine, leading to its accumulation in the synaptic cleft. This accumulation indirectly enhances both muscarinic and nicotinic actions. These agents are classified as reversible or irreversible based on their mechanism of action.     
Irreversible agents form a strong bond with the cholinesterase enzyme, making it inactive. The breakdown of the phosphorylated enzyme is...
779
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

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

850
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...
850
Indirect-Acting Cholinergic Agonists: Pharmacological Actions01:30

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

613
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...
613
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...
1.0K

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

An Overview of In Vitro Release Methods for Long-Acting Injectable Products Based on PLGA.

Methods and protocols·2026
Same author

Heterolysis vs Homolysis and <i>ortho</i>-<i>meta</i>-Effects in the Photohydrolysis of Biphenylamine Photocages.

The Journal of organic chemistry·2026
Same author

Photochemically Assisted Synthesis of Thienobenzotriazole-Based Dual Cholinesterase Inhibitors.

Molecules (Basel, Switzerland)·2025
Same author

Photochemistry-driven design of small molecule cholinesterase ligands.

Chemico-biological interactions·2025
Same author

Charged Thienobenzo-1,2,3-Triazoles as Especially Potent Non-Selective Cholinesterase Inhibitors: Design, Anti-Inflammatory Activity, and Computational Study.

Pharmaceuticals (Basel, Switzerland)·2025
Same author

Heterostilbene Carbamates with Selective and Remarkable Butyrylcholinesterase Inhibition: Computational Study and Physico-Chemical Properties.

Biomolecules·2025

Related Experiment Video

Updated: May 31, 2025

Synthesis of Antiviral Tetrahydrocarbazole Derivatives by Photochemical and Acid-catalyzed C-H Functionalization via Intermediate Peroxides CHIPS
06:34

Synthesis of Antiviral Tetrahydrocarbazole Derivatives by Photochemical and Acid-catalyzed C-H Functionalization via Intermediate Peroxides CHIPS

Published on: June 20, 2014

13.8K

Resveratrol-Based Carbamates as Selective Butyrylcholinesterase Inhibitors: Design, Synthesis, Computational Study

Maja Sviben1, Ilijana Odak2, Danijela Barić3

  • 1Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Trg Marka Marulića 19, HR-10 000 Zagreb, Croatia.

Molecules (Basel, Switzerland)
|January 25, 2025
PubMed
Summary

Researchers developed novel carbamate compounds targeting butyrylcholinesterase (BChE) for neurological disorders. Compounds 1 and 7 show high selectivity and potency, outperforming existing treatments.

Keywords:
ADMETbiometal complexationbutyrylcholinesterase inhibitioncarbamatesdockingmolecular dynamicssynthesis

More Related Videos

Synthetic Methodology for Asymmetric Ferrocene Derived Bio-conjugate Systems via Solid Phase Resin-based Methodology
07:07

Synthetic Methodology for Asymmetric Ferrocene Derived Bio-conjugate Systems via Solid Phase Resin-based Methodology

Published on: March 12, 2015

9.6K
Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor
07:12

Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor

Published on: October 26, 2017

7.8K

Related Experiment Videos

Last Updated: May 31, 2025

Synthesis of Antiviral Tetrahydrocarbazole Derivatives by Photochemical and Acid-catalyzed C-H Functionalization via Intermediate Peroxides CHIPS
06:34

Synthesis of Antiviral Tetrahydrocarbazole Derivatives by Photochemical and Acid-catalyzed C-H Functionalization via Intermediate Peroxides CHIPS

Published on: June 20, 2014

13.8K
Synthetic Methodology for Asymmetric Ferrocene Derived Bio-conjugate Systems via Solid Phase Resin-based Methodology
07:07

Synthetic Methodology for Asymmetric Ferrocene Derived Bio-conjugate Systems via Solid Phase Resin-based Methodology

Published on: March 12, 2015

9.6K
Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor
07:12

Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor

Published on: October 26, 2017

7.8K

Area of Science:

  • Medicinal Chemistry
  • Neuroscience
  • Computational Chemistry

Background:

  • Cholinesterase inhibitors are crucial for treating neurological disorders.
  • Resveratrol analogs have shown promise as cholinesterase inhibitors.
  • Developing selective butyrylcholinesterase (BChE) inhibitors is a key therapeutic goal.

Purpose of the Study:

  • To design and synthesize novel carbamate compounds based on the stilbene skeleton.
  • To evaluate the inhibitory activity and selectivity of these compounds against acetylcholinesterase (AChE) and BChE.
  • To investigate the molecular interactions and ADMET properties of potential drug candidates.

Main Methods:

  • Synthesis of novel carbamate compounds (1-13).
  • In vitro enzyme inhibition assays against AChE and BChE.
  • Molecular docking and molecular dynamics (MD) simulations.
  • Spectrophotometric analysis for metal ion complexation.

Main Results:

  • Compounds 1 and 7 exhibited potent and selective inhibition of BChE (IC50 values of 0.12 ± 0.09 μM and 0.38 ± 0.01 μM, respectively).
  • Inhibitory activity of compounds 1 and 7 surpassed that of galantamine against BChE.
  • Molecular docking and MD simulations revealed favorable interactions and complex stability.
  • Resveratrol-based carbamates showed potential for Fe3+ ion complexation.

Conclusions:

  • Novel carbamates 1 and 7 are highly selective BChE inhibitors.
  • These compounds possess favorable ADMET properties and demonstrate potential as therapeutics for neurological disorders.
  • The study highlights the therapeutic potential of stilbene-based carbamates for neurodegenerative diseases.