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Neuronal Acetylcholine Receptor Alpha4Beta2 Subtype (α4β2 nAChR)
- Target
- α4β2 nAChR
- Molecular classification
- Ligand-gated ion channel, Receptor, Nicotinic acetylcholine receptor (nAChR)
01
Overview
The neuronal acetylcholine receptor alpha4beta2 subtype (α4β2 nAChR) is a ligand-gated ion channel predominantly found in the brain. It is composed of α4 and β2 subunits and plays a crucial role in fast synaptic transmission and cognitive processes. It is the primary target mediating nicotine’s addictive properties, and mutations are linked with epilepsy, growth abnormalities and obesity. It exists primarily in two stoichiometries, (α4)₂(β2)₃ and (α4)₃(β2)₂, each having distinct properties.
- Other names
- alpha4beta2 nAChRα4β2 nicotinic acetylcholine receptorNeuronal Nicotinic Receptor α4β2
02
Mechanism of action
Activation by agonists (acetylcholine, nicotine) opens the ion channel, increasing Na⁺ and K⁺ permeability across the cell membrane, leading to neuronal excitation.
03
Biological functions
Excitatory neurotransmissionModulation of neurotransmitter releaseRegulation of neuronal excitabilityCognitive function (learning, attention)Synaptic plasticity
04
Disease associations
EpilepsyAddictionObesityAutosomal dominant nocturnal frontal lobe epilepsy (ADNFLE)Neurological disorders
05
Safety considerations
Nicotine addictionPotential for seizures with certain mutations/dysfunctionAltered growth patterns with certain mutations
06
Interacting drugs
Acetylcholine
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