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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...

Receptor Downregulation in MVBs

Receptor Downregulation in MVBs

Multivesicular bodies (MVBs) are mature endosomes that sort ubiquitinated proteins and then fuse with lysosomes to degrade the sorted proteins. Epidermal growth factor (EGF) and its receptor (EGFR) form a complex that can be internalized through endocytosis, sorted into an MVB, and later degraded.
The EGFR can initiate signaling pathways that lead to cell proliferation, migration, and differentiation. Overexpression of EGFR stimulates cells to proliferate. Excessive EGFR activation may...

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...

GPCR Desensitization

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...

Receptor-mediated Endocytosis

Receptor-mediated Endocytosis

Receptor-mediated endocytosis is when bulk amounts of specific molecules are imported into a cell after binding to cell surface receptors. The molecules bound to these receptors are taken into the cell through inward folding of the cell surface membrane, which is eventually pinched off into a vesicle within the cell. Structural proteins, such as clathrin, coat the budding vesicle.
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Receptor-mediated Endocytosis

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Related Experiment Video

Updated: May 26, 2026

Tracking Drug-induced Changes in Receptor Post-internalization Trafficking by Colocalizational Analysis

Tracking Drug-induced Changes in Receptor Post-internalization Trafficking by Colocalizational Analysis

Published on: July 3, 2015

Muscarinic receptor trafficking.

Cindy Reiner¹, Neil M Nathanson

¹Department of Pharmacology, University of Washington, 357750, Seattle, WA 98195-7750, USA.

Handbook of Experimental Pharmacology

|January 7, 2012

Summary

Understanding neurotransmitter receptor trafficking is key to regulating cell surface expression. This chapter details muscarinic receptor internalization and degradation, highlighting subtype and cell-specific differences in their trafficking and physiological impacts.

Area of Science:

Neuroscience
Cell Biology
Pharmacology

Background:

Neurotransmitter receptor trafficking regulates cell surface expression and function.
Muscarinic receptors play crucial roles in various physiological processes.
Understanding receptor trafficking is essential for drug development and therapeutic strategies.

Purpose of the Study:

To elucidate the mechanisms governing the internalization and degradation of muscarinic receptors.
To explore receptor subtype-specific and cell-type specific differences in muscarinic receptor trafficking.
To discuss the physiological consequences of muscarinic receptor trafficking.

Main Methods:

Review of studies on muscarinic receptor trafficking in cultured cells.
Analysis of in vivo studies investigating muscarinic receptor dynamics.

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Tracking Drug-induced Changes in Receptor Post-internalization Trafficking by Colocalizational Analysis

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A High-content Assay for Monitoring AMPA Receptor Trafficking

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Integration of data on receptor internalization and degradation pathways.

Main Results:

Muscarinic receptor trafficking exhibits significant subtype-specific variations.
Cell-type specific differences in muscarinic receptor internalization and degradation are evident.
Trafficking mechanisms influence receptor expression and cellular signaling.

Conclusions:

Muscarinic receptor trafficking is a complex process with implications for neuronal function.
Understanding these trafficking mechanisms is vital for targeting muscarinic receptors therapeutically.
Further research into receptor trafficking will advance our knowledge of neurotransmission.