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Related Concept Videos

Cholinergic Receptors: Nicotinic01:15

Cholinergic Receptors: Nicotinic

5.0K
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.
There are two types of nicotinic receptors: neuromuscular (NM/NM/N1) and neuronal (NN/NN/N2). The two families differ based on their location and selectivity to...
5.0K
Cholinergic Receptors: Muscarinic01:25

Cholinergic Receptors: Muscarinic

4.4K
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+....
4.4K
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

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

1.8K
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...
1.8K
Indirect-Acting Cholinergic Agonists: Pharmacological Actions01:30

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

1.3K
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...
1.3K
Cholinergic Neurons: Neurotransmission01:23

Cholinergic Neurons: Neurotransmission

4.8K
Cholinergic neurotransmission involves the synthesis and the release of acetylcholine (ACh) in order to transmit nerve impulses across the synapse. The process begins with the synthesis of acetyl CoA, a precursor for ACh, from ATP, acetate, and coenzyme A in the mitochondria. Choline, another vital precursor, is transported inside the neuron through choline transporters, including high-affinity choline transporter CHT1, low-affinity choline transporter CTL1, and lower-affinity choline...
4.8K
Direct-Acting Cholinergic Agonists: Pharmacological Actions00:59

Direct-Acting Cholinergic Agonists: Pharmacological Actions

2.2K
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...
2.2K

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Related Experiment Video

Updated: Dec 20, 2025

Probing Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices via Laser Flash Photolysis of Photoactivatable Nicotine
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Probing Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices via Laser Flash Photolysis of Photoactivatable Nicotine

Published on: January 25, 2019

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Cholinergic Receptors and Addiction.

Roger L Papke1, Darlene H Brunzell2, Mariella De Biasi3

  • 1Department of Pharmacology and Therapeutics, University of Florida, Gainesville, FL, USA. rlpapke@ufl.edu.

Current Topics in Behavioral Neurosciences
|May 27, 2020
PubMed
Summary

Nicotine addiction involves brain receptors called nicotinic acetylcholine receptors (nAChR). Understanding nAChR subtypes, especially those with β2, α6, and α5 subunits, is key to developing treatments for nicotine and areca nut addiction.

Keywords:
AddictionArecaBetel nutCholinergic receptorsPartial agonistsTobacco

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Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices
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Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices

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Spectral Confocal Imaging of Fluorescently tagged Nicotinic Receptors in Knock-in Mice with Chronic Nicotine Administration
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Spectral Confocal Imaging of Fluorescently tagged Nicotinic Receptors in Knock-in Mice with Chronic Nicotine Administration

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Related Experiment Videos

Last Updated: Dec 20, 2025

Probing Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices via Laser Flash Photolysis of Photoactivatable Nicotine
10:48

Probing Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices via Laser Flash Photolysis of Photoactivatable Nicotine

Published on: January 25, 2019

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Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices
10:04

Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices

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Spectral Confocal Imaging of Fluorescently tagged Nicotinic Receptors in Knock-in Mice with Chronic Nicotine Administration
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Spectral Confocal Imaging of Fluorescently tagged Nicotinic Receptors in Knock-in Mice with Chronic Nicotine Administration

Published on: February 10, 2012

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Addiction Research

Background:

  • Addiction, particularly to tobacco products containing nicotine, is a significant societal issue.
  • Nicotine exerts its effects by interacting with nicotinic acetylcholine receptors (nAChRs) in the brain.
  • nAChRs are ligand-gated ion channels crucial for neurotransmission, especially in reward pathways.

Purpose of the Study:

  • To review the structure and diversity of nAChR subunits.
  • To elucidate the specific roles of different nAChR subtypes in nicotine addiction.
  • To explore the involvement of cholinergic receptors in areca nut addiction and its public health implications.

Main Methods:

  • Review of existing literature on nAChR structure, function, and diversity.
  • Focus on nAChR subtypes containing β2, α6, and α5 subunits.
  • Discussion of homomeric α7 nAChR roles and implications for pharmacotherapy.

Main Results:

  • Specific nAChR subtypes, including those with β2, α6, and α5 subunits, regulate dopamine release in the mesolimbic reward pathway.
  • Homomeric α7 nAChR plays a distinct role in behavioral responses to nicotine.
  • Cholinergic receptors are implicated in areca nut addiction, presenting unique challenges.

Conclusions:

  • Understanding the functional diversity of nAChRs is critical for developing effective pharmacotherapeutic strategies for nicotine addiction.
  • The study highlights the complex neurobiological underpinnings of both nicotine and areca nut addiction.
  • Further research into nAChR subtypes may offer novel avenues for addiction treatment.