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Cholinergic Receptors: Nicotinic

Cholinergic Receptors: Nicotinic

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...

Cholinergic Receptors: Muscarinic

Cholinergic Receptors: Muscarinic

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+. Activation...

Cholinergic Neurons: Neurotransmission

Cholinergic Neurons: Neurotransmission

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...

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

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: Pharmacological Actions

Direct-Acting Cholinergic Agonists: Pharmacological Actions

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...

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

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...

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Related Experiment Video

Updated: May 19, 2026

Localization of Plasma Membrane and Intracellular Neuronal Nicotinic Acetylcholine Receptors Using Quantitative Imaging in Mammalian Cells

Localization of Plasma Membrane and Intracellular Neuronal Nicotinic Acetylcholine Receptors Using Quantitative Imaging in Mammalian Cells

Published on: December 19, 2025

Nicotinic acetylcholine receptors: from basic science to therapeutics.

Raymond Hurst¹, Hans Rollema, Daniel Bertrand

¹Neuroscience Research, Pfizer Worldwide Research and Development, 700 Main Street, Cambridge, MA 02139, USA.

Pharmacology & Therapeutics

|August 29, 2012

Summary

Nicotinic acetylcholine receptors are crucial for neuronal communication and offer therapeutic potential. Research explores their genes, structure, function, and diseases for novel drug development targeting conditions like addiction and Alzheimer's disease.

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

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Localization of Plasma Membrane and Intracellular Neuronal Nicotinic Acetylcholine Receptors Using Quantitative Imaging in Mammalian Cells

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Published on: December 19, 2025

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

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Published on: January 25, 2019

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

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

Published on: October 29, 2012

Area of Science:

Neuroscience
Pharmacology
Molecular Biology

Background:

Neuronal communication relies on neurotransmitter release and signaling, with nicotinic acetylcholine receptors (nAChRs) playing a key role.
nAChRs are ligand-gated ion channels with 16 mammalian genes, forming diverse heteromeric and homomeric subtypes.
The vast subtype combinations of nAChRs present significant opportunities for targeted therapeutic development.

Purpose of the Study:

To review recent insights into nicotinic acetylcholine receptors, covering their genetic basis, structure, function, and associated diseases.
To present the latest findings on the pharmacology of nAChRs and their therapeutic applications.
To analyze the pharmacodynamic and pharmacokinetic properties of nAChR-targeting compounds for clinical translation.

Main Methods:

Review of current literature on nicotinic acetylcholine receptors.
Analysis of genetic, structural, functional, and disease-related data for nAChRs.
Pharmacological evaluation of existing and discontinued nAChR-targeting drug candidates.

Main Results:

Substantial progress has been made in identifying genes and understanding the mechanisms of nAChRs.
The diverse nature of nAChR subtypes offers extensive possibilities for drug design.
Novel chemical entities targeting nAChRs are being explored for various diseases, though few drugs are currently marketed.

Conclusions:

Targeting specific nicotinic acetylcholine receptor subtypes holds promise for treating addiction, depression, ADHD, cognitive deficits, pain, and inflammation.
Further pharmacological analysis is needed to optimize nAChR-targeting molecules and validate therapeutic hypotheses.
Understanding nAChR pharmacology is essential for developing effective treatments for neurological and inflammatory conditions.