Target intelligence / Profile preview

Nicotinic acetylcholine receptor alpha-7 subtype (α7 nAChR)

Target
α7 nAChR
Molecular classification
Ion channel, Receptor, Ligand-gated ion channel
01

Overview

The α7 nicotinic acetylcholine receptor is a ligand-gated ion channel consisting of five identical α7 subunits. It plays critical roles in cognitive functions such as memory and attention, and is implicated in neuroprotection and various diseases. Activation of α7 receptors results in increased calcium influx, which enhances neuronal excitability and neurotransmitter release. This receptor is also involved in inflammatory responses and cancer progression.

Other names
alpha-7 nicotinic receptorα7 receptor
02

Mechanism of action

Activation of α7 receptors leads to increased Ca^2+ permeability, enhancing neuronal excitability and synaptic communication. Agonists like EVP-6124 directly activate the receptor, while positive allosteric modulators like PNU-120596 enhance channel activity.

03

Biological functions

Signal transductionNeuronal excitabilitySynaptic communicationNeuroprotectionCognitive function (memory, learning, attention)
04

Disease associations

Neurodegenerative diseases (Alzheimer's disease, Schizophrenia)CancerCardiovascular diseases (atherosclerosis)InflammationInflammatory neurotoxicity in stroke and myocardial infarction
05

Safety considerations

Potential enhancement of atherosclerosis due to nicotine action on mast cellscareful consideration is needed when using agonists in certain conditions.
06

Interacting drugs

Varenicline

3 more in the full profile.

07

Biomarkers

Increased expression or activity of α7 nAChR can be used as potential biomarkers for some neurological conditions.

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