Target intelligence / Profile preview

Neuronal acetylcholine receptor alpha-3 beta-4 (α3β4 nAChR)

Target
α3β4 nAChR
Molecular classification
Ion channel, Receptor, Ligand-gated ion channel, Cys-loop receptor family
01

Overview

The neuronal acetylcholine receptor alpha-3 beta-4 is a heteropentameric, ligand-gated ion channel found primarily in autonomic ganglia and certain brain regions[4][5]. Composed of alpha-3 (CHRNA3) and beta-4 (CHRNB4) subunits, it enables rapid neurotransmission by opening a cation-permeable channel upon binding acetylcholine or other agonists[1][2][5]. Activation of this receptor leads to sodium and potassium influx, membrane depolarization, and initiation of neuronal excitation, playing a key role in autonomic nervous system communication and some aspects of addiction neurobiology[4][5]. It is studied as a drug target for modulating addiction and autonomic dysfunction; multiple endogenous and exogenous agonists and antagonists are known to interact with the α3β4 nAChR[4][5].

Other names
Alpha-3 beta-4 nicotinic receptorGanglion-type nicotinic receptornAChR α3β4CHRNA3/CHRNB4 receptorα3β4 nicotinic acetylcholine receptor
02

Mechanism of action

Agonist (direct channel opening, e.g., acetylcholine, nicotine); Partial agonist (partial channel opening, e.g., cytisine); Competitive antagonist (blockade of the acetylcholine binding site, e.g., DHβE, SR 16584); Noncompetitive antagonist (allosteric inhibition, e.g., bupropion, mecamylamine, dextromethorphan)

03

Biological functions

Signal transductionNeurotransmission (fast synaptic transmission)Membrane depolarizationResponse to acetylcholineResponse to nicotine
04

Disease associations

Addiction (especially nicotine and other substances)Neurodegenerative disease (implicated in processes)Cardiovascular disease (autonomic regulation)Other (autonomic dysfunction)
05

Safety considerations

Potential for off-target autonomic effects (e.g., hypotension, tachycardia)Risk of addiction (nicotine, other agonists)Central and peripheral nervous system side effects from channel blockade (e.g., seizures, confusion)
06

Interacting drugs

Acetylcholine

20 more in the full profile.

07

Biomarkers

Null (no well-established biomarker use in clinical selection)

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