Target intelligence / Profile preview

Beta-2 Subunit-Containing Nicotinic Acetylcholine Receptor (β2-nAChR)

Target
β2-nAChR
Molecular classification
Ligand-gated ion channel, Cys-loop receptor, Nicotinic acetylcholine receptor, Receptor
01

Overview

The beta-2 subunit-containing nicotinic acetylcholine receptor (β2-nAChR), often referred to as the α4β2 nAChR when paired with the alpha-4 subunit, is a member of the Cys-loop superfamily of ligand-gated ion channels. These receptors are pentameric complexes composed of five transmembrane subunits. The β2 subunit is one of four known neuronal β-type nAChR subunits in mammals. They mediate fast synaptic transmission by allowing cation influx upon activation by acetylcholine or exogenous ligands such as nicotine, playing key roles in neurotransmitter release, synaptic plasticity, attention, learning, memory, and reward pathways. Alterations in expression or function of β2-containing nAChRs have been implicated in cognitive disorders, neurodegenerative diseases, and epilepsy.

Other names
β2-containing nAChRCHRNB2 subunitα4β2 nAChR (when paired with α4)
02

Mechanism of action

Agonist binding leading to cation channel opening and neuronal depolarization

03

Biological functions

Fast synaptic transmissionNeurotransmitter release modulationSynaptic plasticityReward pathway mediationCation channel activity
04

Disease associations

Cognitive disordersNeurodegenerative diseasesEpilepsyAddiction
05

Safety considerations

Potential for addictionSide effects associated with nicotinic receptor agonists/antagonistsInteraction with neurotropic viruses (e.g., rabies virus)
06

Interacting drugs

Acetylcholine

4 more in the full profile.

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