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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...

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...

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic antagonists are called...

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

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...

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...

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Related Experiment Video

Updated: May 28, 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 receptor assays.

¹The Johns Hopkins Medical Institutions, Baltimore, Maryland, USA.

Current Protocols in Pharmacology

|October 4, 2011

Summary

This summary is machine-generated.

This study details methods for pharmacologically analyzing nicotinic acetylcholine receptors (nAChRs) in peripheral tissues. It focuses on isolated preparations to understand nAChR function in autonomic nerves and muscle.

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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: October 29, 2012

Area of Science:

Pharmacology
Neuroscience
Physiology

Background:

Peripheral nicotinic acetylcholine receptors (nAChRs) are primarily located on autonomic nerves and skeletal muscle motor end plates.
Understanding nAChR function is crucial for studying autonomic and neuromuscular signaling.
Existing methods allow for antagonist potency assessment via nerve stimulation or exogenous agonist application.

Purpose of the Study:

To describe and validate experimental preparations for studying peripheral nAChR pharmacology.
To provide techniques for assessing antagonist potencies at autonomic synapses and muscle nAChRs.
To detail methods for evaluating nAChR-mediated responses to exogenous agonists in smooth muscle.

Main Methods:

Utilized isolated guinea pig trachea/esophagus preparation to study nAChRs in parasympathetic and sympathetic nervous system synapses and esophageal striated muscle.
Described a preparation for studying nAChRs in the striated musculature of the diaphragm.
Developed techniques for assessing exogenous nicotinic agonist effects on nAChRs in two smooth muscle preparations.

Main Results:

Successfully demonstrated the utility of the described preparations for pharmacologic analysis of nAChRs.
Provided a framework for quantifying antagonist effects on nAChR-mediated responses in various peripheral tissues.
Established methods applicable to both nerve-stimulated and exogenously stimulated nAChR responses.

Conclusions:

The described experimental models offer robust platforms for detailed pharmacologic characterization of peripheral nAChRs.
These preparations facilitate the study of nAChR function in both neuronal and muscular compartments of the peripheral nervous system.
The methodologies presented are valuable for drug discovery and understanding the role of nAChRs in physiological processes.