Target intelligence / Profile preview

Cholinergic neurotransmission

Molecular classification
Enzyme, G protein-coupled receptor, Ion channel, Transporter
01

Overview

Cholinergic neurotransmission is the physiological process by which the neurotransmitter acetylcholine (ACh) mediates signal transduction across synaptic clefts in both the central and peripheral nervous systems (StatPearls, 2023). This system is fundamental to cognitive processes such as learning, memory, and attention, and it governs the activity of the parasympathetic nervous system and the neuromuscular junction (NIH, 2022). The process involves ACh synthesis by choline acetyltransferase, its storage in vesicles, release into the synapse, and rapid degradation by acetylcholinesterase (AChE) (PubMed, 2021). Dysfunction in cholinergic signaling is central to the pathophysiology of neurodegenerative disorders like Alzheimer's disease and neuromuscular conditions like Myasthenia gravis (Nature Reviews Neuroscience, 2021). Therapeutic strategies often focus on increasing ACh bioavailability through AChE inhibitors or modulating specific muscarinic and nicotinic receptors (Pharmacological Reviews, 2020). While effective, targeting this system can lead to systemic side effects known as cholinergic toxidromes if not precisely managed (StatPearls, 2023).

Other names
Cholinergic systemCholinergic signalingAcetylcholine signaling pathway
02

Mechanism of action

Modulation of acetylcholine levels via acetylcholinesterase inhibition or direct activation/blockade of muscarinic and nicotinic receptors (StatPearls, 2023; PubMed, 2021).

03

Biological functions

Signal transductionNeuromuscular transmissionCognitive functionAutonomic nervous system regulationMemoryArousal
04

Disease associations

Alzheimer's diseaseMyasthenia gravisParkinson's diseaseGlaucomaSchizophreniaNeurodegenerative disease
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Safety considerations

Cholinergic crisisSLUDGE syndrome (Salivation, Lacrimation, Urination, Defecation, GI distress, Emesis)BradycardiaBronchospasmMuscle fasciculationsNausea and vomiting
06

Interacting drugs

Donepezil

8 more in the full profile.

07

Biomarkers

Acetylcholinesterase activityCerebrospinal fluid acetylcholine levelsPET imaging of vesicular acetylcholine transporter (VAChT)

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