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Related Concept Videos

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

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

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...
Indirect-Acting Cholinergic Agonists: Mechanism of Action01:18

Indirect-Acting Cholinergic Agonists: Mechanism of Action

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, leading to...
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

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

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...
Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

Direct-Acting Cholinergic Agonists: Pharmacokinetics

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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Related Experiment Video

Updated: May 29, 2026

Novel Atomic Force Microscopy Based Biopanning for Isolation of Morphology Specific Reagents against TDP-43 Variants in Amyotrophic Lateral Sclerosis
13:31

Novel Atomic Force Microscopy Based Biopanning for Isolation of Morphology Specific Reagents against TDP-43 Variants in Amyotrophic Lateral Sclerosis

Published on: February 12, 2015

Virtual screening against acetylcholine binding protein.

Maleeruk Utsintong1, Piyanuch Rojsanga, Kwok-Yiu Ho

  • 1School of Pharmaceutical Sciences, University of Phayao, Phayao, Thailand.

Journal of Biomolecular Screening
|September 30, 2011
PubMed
Summary
This summary is machine-generated.

Researchers identified novel compounds targeting nicotinic acetylcholine receptors (nAChRs). These potential drug candidates show promise for developing new treatments for neurological disorders by acting as selective antagonists or partial agonists.

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Studies of Chaperone-Cochaperone Interactions using Homogenous Bead-Based Assay
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Studies of Chaperone-Cochaperone Interactions using Homogenous Bead-Based Assay

Published on: July 21, 2021

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Last Updated: May 29, 2026

Novel Atomic Force Microscopy Based Biopanning for Isolation of Morphology Specific Reagents against TDP-43 Variants in Amyotrophic Lateral Sclerosis
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Published on: February 12, 2015

Studies of Chaperone-Cochaperone Interactions using Homogenous Bead-Based Assay
06:51

Studies of Chaperone-Cochaperone Interactions using Homogenous Bead-Based Assay

Published on: July 21, 2021

Area of Science:

  • Neuroscience
  • Pharmacology
  • Structural Biology

Background:

  • Nicotinic acetylcholine receptors (nAChRs) are crucial for neural communication.
  • The α(7) acetylcholine binding protein (AChBP) structure is a key template for nAChR drug discovery.

Purpose of the Study:

  • To identify novel compounds targeting the α(7) nicotinic acetylcholine receptor.
  • To explore potential therapeutic scaffolds for modulating nAChR activity.

Main Methods:

  • Virtual screening of the National Cancer Institute diversity set against AChBP using AutoDock.
  • In vitro radioligand competition assays with radiolabeled epibatidine.
  • Functional assays using Xenopus oocytes and FRET-based calcium sensors in HEK cells.

Main Results:

  • 51 potential drug candidates were identified via virtual screening.
  • Seven compounds exhibited micromolar to nanomolar affinities for AChBPs.
  • Two compounds (NSC36369 and NSC34352) demonstrated selective antagonism of α(7)nAChR.

Conclusions:

  • Identified compounds serve as novel scaffolds for developing potent and specific nAChR modulators.
  • NSC34352 exhibits partial agonistic effects at low doses, indicating complex activity.
  • The study provides valuable leads for future drug development targeting nAChRs.