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Related Concept Videos

Cholinergic Receptors: Muscarinic01:25

Cholinergic Receptors: Muscarinic

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The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine. 
The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+....
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Nicotinic receptors are ligand-gated ion channels that are activated by acetylcholine and nicotine. Upon activation, they cause a rapid increase in the permeability of cells to K+, Na+, and Ca2+, followed by depolarization and excitation. They are in the autonomic ganglia, skeletal neuromuscular junction, CNS, and adrenal medulla.
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Cooperative Allosteric Transitions01:58

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Cooperative allosteric transitions can occur in multimeric proteins, where each subunit of the protein has its own ligand-binding site. When a ligand binds to any of these subunits, it triggers a conformational change that affects the binding sites in the other subunits; this can change the affinity of the other sites for their respective ligands. The ability of the protein to change the shape of its binding site is attributed to the presence of a mix of flexible and stable segments in the...
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Allosteric Regulation01:08

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Allosteric regulation of enzymes occurs when the binding of an effector molecule to a site that is different from the active site causes a change in the enzymatic activity. This alternate site is called an allosteric site, and an enzyme can contain more than one of these sites. Allosteric regulation can either be positive or negative, resulting in an increase or decrease in enzyme activity. Most enzymes that display allosteric regulation are metabolic enzymes involved in the degradation or...
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Related Experiment Video

Updated: Jan 30, 2026

A Tissue Displacement-based Contusive Spinal Cord Injury Model in Mice
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Positive Allosteric Modulation of Cholinergic Receptors Improves Spatial Learning after Cortical Contusion Injury in

Daniel P Holschneider1,2,3, Yumei Guo1, Zhuo Wang1

  • 11 Department of Psychiatry and the Behavioral Sciences and Biomedical Engineering, University of Southern California, Los Angeles, California.

Journal of Neurotrauma
|January 29, 2019
PubMed
Summary

Benzyl quinolone carboxylic acid (BQCA) improved spatial recall in mice with brain trauma. This M1 muscarinic-positive allosteric modulator enhanced memory function without significant motor side effects.

Keywords:
acetylcholinecerebral metabolismcholinergiccortical contusion injurymemorymicemotor functionpositive allosteric modulatorsspatial navigationtraumatic brain injury

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Neurology

Background:

  • Cerebral cortical contusion injury (CCI) causes memory deficits and motor dysfunction.
  • M1 muscarinic-positive allosteric modulators are being investigated for neurological recovery.

Purpose of the Study:

  • To evaluate the efficacy of benzyl quinolone carboxylic acid (BQCA) in improving memory and motor deficits following CCI in mice.
  • To assess the impact of BQCA on cerebral metabolic activity in CCI models.

Main Methods:

  • Adult mice underwent unilateral motor-sensory cortical CCI or sham injury.
  • Mice were treated with BQCA (5, 10, 20 mg/kg) or vehicle, with weekly motor and spatial learning tests (Morris water maze).
  • Cerebral metabolic activation was measured using [14C]-2-deoxyglucose autoradiography and analyzed with statistical parametric mapping.

Main Results:

  • CCI mice exhibited motor deficits and impaired spatial learning.
  • BQCA treatment significantly improved spatial recall in CCI mice, with minimal impact on motor function.
  • CCI reduced local cerebral glucose uptake (rCGU) in specific brain regions; BQCA partially reversed these changes and increased rCGU in motor areas.

Conclusions:

  • BQCA demonstrates potential as a therapeutic agent for improving learning and memory after brain trauma.
  • BQCA may offer an alternative to other cholinergic enhancers, potentially avoiding common central nervous system side effects.