

CHO-K1 Human nAChR α3β4α5 Stable Cell
Item | Cat# | Price |
Stable Cell Line | SNB-I-0030A | $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 α3β4α5 cell line express non-tag full length human nAChR receptor α3 α5 and β4 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_000743 (α3), NM_000750 (β4), NM_000745 (α5) |
Parental Line | CHO-K1 |
Lot# | See Vial |
Storage | Liquid Nitrogen |
Data
![Human nAChR α3β4α5 Activator Assay. CHO-K1 Human nAChR α3β4α5 cell were seeded in 384-well plate and incubated at 37oC in 5% CO2 incubator for 24 hours before running the assay. The cells were treated with the reference activator. The assay was run based on FLIPR membrane potential assay protocol. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.](https://static.wixstatic.com/media/cbf7de_83158ebc687b4ea7991e8266476a8f7a~mv2.png/v1/fill/w_75,h_75,al_c,q_85,usm_0.66_1.00_0.01,blur_2,enc_auto/cbf7de_83158ebc687b4ea7991e8266476a8f7a~mv2.png)
Target Background
The nicotinic acetylcholine receptor (nAChR) subtype α3β4α5 is a heteromeric ligand-gated ion channel belonging to the Cys-loop receptor family. It is composed of α3, β4, and α5 subunits, encoded respectively by the CHRNA3, CHRNB4, and CHRNA5 genes, which are clustered together on human chromosome 15q25. This receptor configuration is widely expressed in the autonomic nervous system—especially in sympathetic and parasympathetic ganglia—as well as in the central nervous system, including the medial habenula and interpeduncular nucleus.
Functionally, α3β4α5 receptors mediate rapid cholinergic neurotransmission by converting acetylcholine or nicotine binding into the opening of a non-selective cation channel permeable to Na⁺, K⁺, and Ca²⁺. The incorporation of the α5 subunit does not form a receptor on its own but acts as an accessory subunit that modulates the biophysical and pharmacological properties of the α3β4 core receptor. Specifically, α5 inclusion enhances calcium permeability, alters desensitization kinetics, and increases current amplitude, thereby fine-tuning synaptic strength and neuronal excitability.
Physiologically, the α3β4α5 receptor complex plays a crucial role in regulating autonomic ganglionic transmission, cardiovascular function, and stress responses. In the brain, it contributes to habenulo-interpeduncular signaling pathways that modulate reward, aversion, and nicotine dependence. Genetic polymorphisms in CHRNA5-CHRNA3-CHRNB4 are strongly associated with nicotine addiction, lung cancer susceptibility, and other neuropsychiatric conditions.
Because of its restricted localization and unique modulatory role, the α3β4α5 receptor has become an important pharmacological target for developing therapies aimed at treating addiction, chronic pain, and autonomic dysfunction with improved specificity and reduced systemic side effects.