Target intelligence / Profile preview

Neuronal nicotinic acetylcholine receptor α3β4 (nAChR α3β4)

Target
nAChR α3β4
Molecular classification
Ligand-gated ion channel, Ion channel, Receptor
01

Overview

The **neuronal nicotinic acetylcholine receptor α3β4** is a pentameric ligand-gated ion channel composed of α3 and β4 subunits, predominantly expressed in the peripheral nervous system and select regions of the central nervous system. Upon binding acetylcholine or other agonists, it opens to form a cation-selective channel, enabling rapid synaptic transmission. This receptor subtype contributes to the modulation of neurotransmitter release, neuronal excitability, and autonomic function. The genes encoding the α3 and β4 subunits (CHRNA3, CHRNB4) are closely clustered in the genome and have been implicated by genetic association studies as risk factors for nicotine dependence, certain pulmonary diseases, and various other pathologies. The α3β4 receptor is a therapeutic target for smoking cessation and other neuropharmacological interventions, but its peripheral and central expression raise safety concerns, especially regarding cardiovascular and addiction-related side effects[1][2][3][4][5][6].

Other names
α3β4 nicotinic acetylcholine receptorneuronal nAChR α3β4nAChR α3β4CHRNA3/CHNRB4 receptorneuronal acetylcholine receptor subunit alpha-3/beta-4
02

Mechanism of action

Agonists activate the receptor, opening the ion channel to allow cation influx (Na⁺, K⁺, Ca²⁺), leading to membrane depolarization and downstream signaling Antagonists bind and block the receptor, preventing activation by acetylcholine or other agonists

03

Biological functions

Signal transductionRegulation of neurotransmitter releaseModulation of neuronal excitabilitySynaptic transmissionCell integration and networking
04

Disease associations

Neurodegenerative diseaseAddiction (nicotine dependence)Lung cancerChronic obstructive pulmonary disease (COPD)Peripheral arterial diseaseAlcoholism
05

Safety considerations

Blood pressure modulation and autonomic nervous system side effects due to widespread peripheral expressionRisk of addiction and central nervous system side effects with agonists (nicotine, cytisine)Cardiovascular risk, especially with chronic exposure to nicotinePotential for off-target toxicity in non-neuronal cells
06

Interacting drugs

Nicotine

6 more in the full profile.

07

Biomarkers

Genetic variants in CHRNA3 and CHRNB4 gene cluster as risk factors for nicotine dependence, lung cancer, and COPD

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