Target intelligence / Profile preview

Neuronal acetylcholine receptor subunit alpha-7 (α7 nAChR) (α7 nAChR)

Target
α7 nAChR
Molecular classification
Ion channel, Ligand-gated ion channel, Nicotinic acetylcholine receptor
01

Overview

The neuronal alpha-7 nicotinic acetylcholine receptor (α7 nAChR) is a homopentameric ligand-gated ion channel widely expressed in the central nervous system, particularly in the hippocampus and cerebral cortex (UniProt P36544). It is distinguished by its high permeability to calcium ions and rapid desensitization kinetics, playing a pivotal role in modulating neurotransmitter release, synaptic plasticity, and long-term potentiation (PMID: 28935558). Beyond its neuronal functions, the α7 nAChR is a key component of the cholinergic anti-inflammatory pathway, where its activation on macrophages inhibits the release of pro-inflammatory cytokines (PMID: 22433054). In disease states, reduced expression or dysfunction of this receptor is strongly linked to cognitive deficits in schizophrenia and Alzheimer's disease (StatPearls NBK531483). Consequently, it is a major therapeutic target for pro-cognitive drugs, including agonists and positive allosteric modulators, which aim to restore cholinergic tone and enhance cognitive performance (PMID: 25159936).

Other names
CHRNA7Alpha-7 nicotinic cholinergic receptorNicotinic acetylcholine receptor alpha-7 subunitCholinergic receptor nicotinic alpha 7 subunit
02

Mechanism of action

Agonism, partial agonism, and positive allosteric modulation (PAM) to enhance cholinergic signaling and calcium influx.

03

Biological functions

Signal transductionSynaptic transmissionCalcium signalingNeuroprotectionImmune response
04

Disease associations

Alzheimer's diseaseSchizophreniaCognitive impairmentInflammationNeurodegenerative disease
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Safety considerations

Rapid receptor desensitizationGastrointestinal side effectsPotential for seizures at high dosesSelectivity over other nicotinic subtypes
06

Interacting drugs

Varenicline

5 more in the full profile.

07

Biomarkers

P50 sensory gating[18F]ASEM PET imagingMATRICS Consensus Cognitive Battery (MCCB)

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