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Related Concept Videos

Cholinergic Receptors: Nicotinic01:15

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...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
Ligand-gated Ion Channels01:19

Ligand-gated Ion Channels

Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that include the...
Ligand-gated Ion Channels01:19

Ligand-gated Ion Channels

Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that include the...
Drugs Acting on Autonomic Ganglia: Stimulants01:23

Drugs Acting on Autonomic Ganglia: Stimulants


Ganglionic stimulants activate NM nicotinic receptors in autonomic ganglia, falling into two categories: nicotine mimetics [e.g., lobeline, dimethylpiperazine, tetramethylammonium] and muscarinic receptor agonists [e.g., muscarine, methacholine]. The first category's action is rapid and blocked by nicotinic receptor antagonists, while the second category's action is delayed and blocked by atropine-like agents. Nicotine, an alkaloid, affects the heart rate by stimulating sympathetic or...
Cholinergic Receptors: Muscarinic01:25

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...

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Updated: Jul 17, 2026

Localization of Plasma Membrane and Intracellular Neuronal Nicotinic Acetylcholine Receptors Using Quantitative Imaging in Mammalian Cells
09:06

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

Published on: December 19, 2025

Central nicotinic receptors: structure, function, ligands, and therapeutic potential.

M Novella Romanelli1, Paola Gratteri, Luca Guandalini

  • 1Laboratory of Design, Synthesis, and Study of Biologically Active Heterocycles (HeteroBioLab), Department of Pharmaceutical Sciences, University of Florence, via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy. novella.romanelli@unifi.it

Chemmedchem
|February 14, 2007
PubMed
Summary

Researchers are developing new ligands to understand nicotinic receptors (nAChRs) involved in CNS diseases. This review covers novel agonists, antagonists, and allosteric modulators, aiding drug discovery for neurological conditions.

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

  • Neuroscience
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Nicotinic receptors (nAChRs) are widely expressed in neuronal and non-neuronal tissues and implicated in central nervous system (CNS) pathologies.
  • nAChRs are highly heterogeneous membrane proteins with incomplete structural and compositional data.
  • A lack of selective ligands hinders the study of nAChR roles in physiological and pathological conditions.

Purpose of the Study:

  • To review novel agonists, antagonists, and allosteric ligands for nicotinic receptors.
  • To highlight current knowledge on binding site models for designing new compounds.
  • To discuss nicotinic acetylcholine receptor (nAChR) modulators that have advanced to clinical trials.

Main Methods:

  • Literature review of scientific publications and clinical trial data.
  • Analysis of ligand design strategies, including natural product-derived compounds and high-throughput screening.
  • Focus on molecular modeling approaches for binding site analysis.

Main Results:

  • Synthesis of numerous ligands targeting nicotinic receptors, with some selectivity achieved (e.g., between alpha4beta2 and alpha7 subtypes).
  • Advancements in understanding nAChR structure and function through novel ligand development.
  • Identification of nAChR modulators that have progressed into clinical trials for various CNS conditions.

Conclusions:

  • Novel ligands and molecular modeling are crucial for advancing the study of nicotinic receptors.
  • Continued research into nAChR modulators holds promise for treating CNS disorders.
  • The development of selective ligands is key to elucidating nAChR functions in health and disease.