CHO-K1 Human nAChR α4β2α5 Stable Cell
Item | Cat# | Price |
Stable Cell Line | SNB-I-0032A | $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 α4β2α5 cell line express non-tag full length human nAChR receptor α4, α5 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), NM_000745(α5) |
Parental Line | CHO-K1 |
Lot# | See Vial |
Storage | Liquid Nitrogen |
Data
Target Background
The nicotinic acetylcholine receptor (nAChR) subtype α4β2α5 is a heteromeric ligand-gated ion channel belonging to the Cys-loop receptor superfamily. It is formed by the assembly of α4, β2, and α5 subunits, encoded by the CHRNA4, CHRNB2, and CHRNA5 genes, respectively. The α5 subunit acts as an accessory, non-ligand-binding subunit that modulates the receptor’s functional and pharmacological properties without directly forming the acetylcholine binding site.
The α4β2α5 receptor subtype is predominantly expressed in the central nervous system, including the cerebral cortex, hippocampus, thalamus, and interpeduncular nucleus. Functionally, it mediates fast excitatory neurotransmission by coupling acetylcholine or nicotine binding to the opening of a non-selective cation channel permeable to Na⁺, K⁺, and Ca²⁺. Compared with the α4β2 receptor, incorporation of the α5 subunit increases calcium permeability, enhances current amplitude, and alters desensitization kinetics, thereby influencing neuronal excitability and synaptic plasticity.
Physiologically, α4β2α5 receptors play critical roles in attention, cognition, arousal, and reward processing. Their high sensitivity to nicotine makes them key mediators of nicotine’s reinforcing effects in the brain. Genetic variations in CHRNA5—particularly the rs16969968 polymorphism—have been strongly linked to nicotine dependence, smoking behavior, and susceptibility to related diseases such as chronic obstructive pulmonary disease and lung cancer.
Pharmacologically, the α4β2α5 receptor has attracted significant interest as a therapeutic target for neuropsychiatric and cognitive disorders. Selective modulators that fine-tune α4β2α5 receptor activity are being explored for potential applications in nicotine addiction, Alzheimer’s disease, schizophrenia, and attention-deficit disorders, aiming to enhance cognitive function while minimizing side effects.