Target intelligence / Profile preview

Nicotinic Acetylcholine Receptor Alpha3Beta4 (α3β4 nAChR)

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

Overview

The nicotinic acetylcholine receptor alpha3beta4 (α3β4 nAChR) is a subtype of neuronal nicotinic acetylcholine receptors, which are pentameric ligand-gated ion channels. These receptors mediate fast synaptic transmission by allowing cation flux across the cell membrane upon activation by agonists such as acetylcholine or nicotine. It is predominantly expressed in autonomic ganglia and specific brain regions involved in reward circuits and addiction pathways. The α3β4 receptor is implicated in drug-seeking behavior, making it an attractive target for anti-addiction therapies.

Other names
alpha3beta4 nAChRα3β4 nicotinic receptornAChR α3β4
02

Mechanism of action

Activation leads to increased permeability to Na+ and K+, resulting in post-synaptic excitation. Antagonists block the receptor at the orthosteric site or allosterically, preventing ion channel opening.

03

Biological functions

NeurotransmissionSignal transductionRegulation of autonomic functionsModulation of reward pathways
04

Disease associations

Substance use disorderAddictionLung cancer susceptibility
05

Safety considerations

Non-selective targeting can lead to side effects due to the broad distribution of other nAChR subtypes.Potential for cardiovascular effects due to autonomic nervous system involvement.
06

Interacting drugs

Acetylcholine

21 more in the full profile.

07

Biomarkers

Genetic variations in CHRNA3/CHRNA5/CHRNB4 gene cluster associated with smoking behavior and lung cancer risk

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