Target intelligence / Profile preview

Neuronal acetylcholine receptor subunit alpha-7 (CHRNA7)

Target
CHRNA7
Molecular classification
Ion channel, Ligand-gated ion channel, Cys-loop receptor, Receptor
01

Overview

Neuronal acetylcholine receptor subunit alpha-7 is a homopentameric ligand-gated ion channel, part of the Cys-loop receptor family. It is highly expressed in the central nervous system and some peripheral tissues, where it mediates fast synaptic cholinergic transmission, is highly permeable to calcium ions, and regulates neuronal excitability, synaptic plasticity, inflammation, and cell proliferation. CHRNA7 plays key roles in cognition and is involved in pathologies such as Alzheimer’s disease, schizophrenia, cancer, and sepsis. Its pharmacology features rapid desensitization and unique gating properties, and it is targeted by drugs such as nicotine, Varenicline, epibatidine, α-bungarotoxin, and positive allosteric modulators. The α7 subtype is distinguished by singular calcium permeability and is a focus for therapeutic intervention in neurodegenerative, cardiovascular, and inflammatory diseases.

Other names
Alpha-7 nicotinic acetylcholine receptorα7 nicotinic receptorα7 nAChRα7 receptorCholinergic receptor nicotinic alpha 7 subunitCHRNA7
02

Mechanism of action

Agonists activate the receptor to facilitate cation (mainly Ca^2+) flow, increase synaptic transmission, and modulate inflammatory response. Antagonists block ion channel gating. Positive allosteric modulators enhance receptor activation and channel conductance.

03

Biological functions

Signal transductionSynaptic transmission (cholinergic, dopaminergic)Calcium ion transport and homeostasisCognitive functions (memory, learning, attention)Regulation of inflammationCell proliferationRegulation of membrane potentialNeuronal action potentialDopamine biosynthesisAngiogenesisCell death/survivalApoptosisImmune response (e.g., B cell and T cell activation)
04

Disease associations

Neurodegenerative disease (Alzheimer’s disease)Inflammation (cholinergic anti-inflammatory pathway, sepsis)Cancer (cell proliferation, metastasis)Cardiovascular disease (myocardial infarction, atherosclerosis)Psychiatric disorders (schizophrenia, cognitive impairment)Stroke
05

Safety considerations

Rapid desensitization (limits duration of drug effects)Nonselective activation can affect multiple neurotransmitter systemsPotential for neurotoxicity at high activationDrug interactions (notably with other nAChR subtypes)
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Interacting drugs

Varenicline

5 more in the full profile.

07

Biomarkers

α7-nAChR protein expression (often upregulated in response to disease states or drug treatment)Response to Varenicline in smoking cessation therapyExpression level in tumors (cancer biomarker)

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