CHO-K1 Human nAChR α4β2 Stable Cell
Item | Cat# | Price |
Stable Cell Line | SNB-I-0031A | $19,800 |
Compound Test Services | CT-001 | $1,850 per 384w plate (Up To 16 cpds Dose) |
Product Description
The nicotinic acetylcholine receptor (nAChR) is a ligand-gated ion channel that mediates fast synaptic transmission at the neuromuscular junction and in the central and peripheral nervous systems. It is activated by the neurotransmitter acetylcholine (ACh) as well as exogenous agonists such as nicotine. Structurally, nAChRs are pentameric complexes composed of five subunits (typically combinations of α, β, γ, δ, or ε), forming a central pore permeable to cations including sodium, potassium, and calcium. Upon ACh binding to the α subunits, the receptor undergoes conformational changes that open the ion channel, leading to depolarization and subsequent action potential generation. In skeletal muscle, nAChRs are essential for muscle contraction, while in the brain they modulate neurotransmitter release, attention, learning, and reward pathways. Dysregulation of nAChR function has been implicated in various disorders such as myasthenia gravis, Alzheimer’s disease, schizophrenia, and nicotine addiction, making it an important therapeutic target.
Screeningbio’s nAChR α4β2 cell line express non-tag full length human nAChR receptor α4 and β2 subunit in CHO-K1 cell. When activated, cell line response to extracellular stimuli (e.g. nicotine) and result in channel opening and membrane potential change. Change of membrane potential was detected by membrane potential sensitive dye.
Product Specifications
Target Type | Ion Channel |
Species | Human |
HGNC Symbol | nAChR |
Accession Number | NM_000744(α4), NM_000748(β2) |
Parental Line | CHO-K1 |
Lot# | See Vial |
Storage | Liquid Nitrogen |
Data
Target Background
The nicotinic acetylcholine receptor (nAChR) subtype α4β2 is one of the most abundant and functionally significant nicotinic receptor subtypes in the mammalian central nervous system. It is a heteromeric ligand-gated ion channel formed by the assembly of α4 and β2 subunits, encoded by the CHRNA4 and CHRNB2 genes. Depending on the stoichiometry of its subunit composition, α4β2 receptors can exist as either (α4)₂(β2)₃ or (α4)₃(β2)₂ pentamers, which differ in agonist sensitivity, ion permeability, and desensitization kinetics.
The α4β2 nAChR mediates fast excitatory neurotransmission through the binding of acetylcholine or nicotine, leading to the opening of a non-selective cation channel permeable to Na⁺, K⁺, and Ca²⁺. The high-sensitivity (α4)₂(β2)₃ form responds to low micromolar nicotine concentrations, while the low-sensitivity (α4)₃(β2)₂ form requires higher concentrations and exhibits slower desensitization. This dual-state behavior allows α4β2 receptors to finely regulate neuronal excitability and synaptic plasticity under varying cholinergic tone.
Anatomically, α4β2 receptors are highly expressed in the cortex, hippocampus, thalamus, and midbrain dopaminergic neurons, where they modulate attention, arousal, learning, and reward circuits. They are the principal targets of nicotine in the brain, mediating both its addictive and cognitive-enhancing effects.
Clinically, dysregulation of α4β2 receptor function is implicated in neuropsychiatric and neurodegenerative disorders such as Alzheimer’s disease, Parkinson’s disease, schizophrenia, and nicotine dependence. Consequently, α4β2 receptors are a major therapeutic target for cognitive enhancement and smoking cessation, with partial agonists such as varenicline specifically designed to modulate this receptor subtype.