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CHO-K1 Human nAChR α3β4 Stable Cell

Item
Cat#
Price

Stable Cell Line

SNB-I-0029A

$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 α3β4 cell line express non-tag full length human nAChR receptor α3 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)

Parental Line

CHO-K1

Lot#

See Vial

Storage

Liquid Nitrogen


Data

Human nAChR α3β4 Activator Assay. CHO-K1 Human nAChR α3β4 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.
Human nAChR α3β4 Activator Assay. CHO-K1 Human nAChR α3β4 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.


Target Background



The nicotinic acetylcholine receptor (nAChR) subtype α3β4 is a heteromeric ligand-gated ion channel belonging to the Cys-loop receptor superfamily. It is formed by the assembly of α3 and β4 subunits, encoded by the CHRNA3 and CHRNB4 genes, respectively. This receptor subtype is widely expressed in the peripheral nervous system, particularly in autonomic ganglia, as well as in selected regions of the central nervous system such as the medial habenula and interpeduncular nucleus.


Functionally, the α3β4 nAChR mediates fast synaptic transmission by converting the binding of acetylcholine or nicotine into the opening of a non-selective cation channel permeable to Na⁺, K⁺, and Ca²⁺. Compared with other nAChR subtypes, α3β4 receptors display lower sensitivity to nicotine but higher calcium permeability, enabling them to influence neuronal excitability, neurotransmitter release, and intracellular signaling cascades. Their rapid activation and desensitization kinetics make them critical for regulating the strength and timing of cholinergic neurotransmission in ganglionic synapses.


Physiologically, α3β4 receptors play essential roles in autonomic control, including cardiovascular regulation, gastrointestinal motility, and stress responses. In the central nervous system, they are involved in reward pathways and aversive behavior modulation. Dysregulation or genetic variation of α3β4 nAChRs has been linked to nicotine dependence, neuropathic pain, and certain neuropsychiatric disorders.

Due to their selective distribution and pharmacological profile, α3β4 receptors have become attractive drug targets for conditions such as addiction, depression, and pain management, with efforts focusing on subtype-specific agonists, partial agonists, and antagonists to achieve precise neuromodulation with minimal side effects.

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