Target intelligence / Profile preview

Nicotinic Acetylcholine Receptor α4α6β2 (nAChR α4α6β2)

Target
nAChR α4α6β2
Molecular classification
Ligand-gated ion channel, Receptor, Nicotinic Acetylcholine Receptor
01

Overview

The nicotinic acetylcholine receptor (nAChR) α4α6β2 is a subtype of neuronal nAChRs, which are pentameric ligand-gated ion channels. These receptors respond to the neurotransmitter acetylcholine and the exogenous agonist nicotine. The nAChR α4α6β2 subtype is a heteromeric pentamer composed primarily of combinations of α4, α6, and β2 subunits, and is selectively expressed in dopaminergic and noradrenergic neurons. Activation induces prolonged depolarization that influences dopamine release, making it a key player in reward signaling and addiction. Its dysfunction has been implicated in addiction, Parkinson’s disease, neuropsychiatric disorders, and cognitive dysfunctions, making it a therapeutic target.

Other names
α4α6β2 nAChRα4α6β2 nicotinic receptorNicotinic receptor α4α6β2 subtype
02

Mechanism of action

Agonist-induced cation channel opening leading to neuronal depolarization and downstream effects on neurotransmitter release. Antagonists block agonist binding and channel activation.

03

Biological functions

Synaptic transmissionNeuromodulationRegulation of dopamine releaseCation channel activity
04

Disease associations

AddictionParkinson’s diseaseNeuropsychiatric disordersCognitive dysfunctionsNeurodegenerative disease
05

Safety considerations

Potential for addictionSide effects related to altered dopaminergic and noradrenergic signalingOff-target effects on other nAChR subtypes
06

Interacting drugs

Acetylcholine

2 more in the full profile.

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