Ion Channel Screening Technologies and Platforms
Ion channels play essential roles in many physiological processes including cell signal transduction, membrane potential, neurotransmission and cardiac muscle contraction. Ion channels are also therapeutic targets of many drugs, in particular central nervous system (CNS) drug development.
Creative Biolabs endeavors to provide ion channel screening service with best-in-class quality and high throughput to cover a wide range of applications such as neuroscience, CNS disease, tumor and drug safety evaluation.
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Technical Highlights
Multi-platform technology integration
Combining automated patch clamp, electrophysiological detection, fluorescence imaging, multi-electrode arrays (MEA), and membrane potential-sensitive probe technologies to achieve multi-dimensional, high-throughput screening.
Broad coverage of ion channel targets
Supports over 30 mainstream ion channels, including those related to neuroscience, immunology, and oncology.
Customized screening solutions
Flexibly designs experimental protocols based on customer requirements, including channel selection, dose settings, and data output formats.
Strict quality control
Adheres to standard operating procedures (SOPs) throughout the entire process, with quality control standards established for critical steps to ensure data comparability and reproducibility.
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What is Ion Channel Screening?
Ion channel screening is a powerful tool for researchers to screen drug candidates that target ion channels, as well as their safety and specificity. Ion channels are transmembrane proteins of the cell membrane which are responsible for regulating the flow of specific ions such as sodium (Na+), potassium (K+), calcium (Ca2+) and chloride (Cl-). Ion channels have been known to be involved in the modulation of many physiological processes, including the transmission of neural signals, or the contraction of cardiac muscles. Ion channels have been shown to be targets for drugs to treat a wide variety of diseases, such as neurological, cardiovascular diseases, and pain.
Ion Channel Screening and Profiling Services
With our advanced platform and extensive experience, Creative Biolabs is confident in providing the best ion channel screening services, including
In recent years, two main and highly complementary strategies have formed the basis of cell-based ion channel screening:
- High-throughput optical analysis
- Higher-throughput electrophysiological methods
These methods provide an efficient and integrated workflow for ion channel drug discovery. We provide ion channel screening services including:
- Patch clamp detection technology based on electrophysiological principles to record changes in current or voltage.
- Real-time fluorescence imaging technology based on non-electrophysiological principles to monitor changes in intracellular calcium concentration, potassium ion concentration, or cell membrane potential.
These assays can be performed in primary cells from different species, iPSC-induced differentiated cells, stably transfected cell lines, and transiently transfected cells. Our strengths lie in our high-throughput screening technology and traditional patch clamp technology, offering multiple options to meet customers' diverse needs and providing data quickly and with high quality.
Patch Clamp System
The patch-clamp technique is a groundbreaking electrophysiological method that enables the recording of ionic currents through individual or small groups of ion channels in cell membranes.
| Recording Mode | Description | Key Features | Typical Applications |
|---|---|---|---|
| Cell-Attached | Pipette forms a tight seal on a small patch of intact cell membrane without breaking it. | Preserves intracellular environment; records single-channel activity. | Study of single ion channel behavior in native conditions. |
| Whole-Cell | Strong suction ruptures the membrane patch under the pipette, allowing electrical access to the entire cell. | Measures total ionic currents across the whole cell membrane. | Analysis of whole-cell electrophysiology and cellular responses. |
| Inside-Out Patch | After seal formation, the pipette is retracted to pull a membrane patch away, exposing the intracellular side to bath solution. | Enables manipulation of intracellular environment; study of intracellular modulators. | Investigation of intracellular signaling and channel regulation. |
| Outside-Out Patch | Starting from whole-cell mode, pipette is withdrawn causing membrane to reseal with extracellular side exposed. | Allows study of extracellular ligand effects on ion channels. | Pharmacological testing of ligand-gated ion channels. |
Figure 1 Illustration of main patch-clamp recording configurations.1,4
Patch clamp is an extremely versatile technique used commonly in neuroscience, cardiology, pharmacology and cell biology. This technique allows for the study of ion channel behavior in both native and heterologous systems.
Fluorescence-Based Screening
Fluorescence membrane potential detection technology is a high-throughput technology that uses changes in fluorescence signals to detect cell membrane potential dynamics in real time. Its process is shown below:
Common probe types are:
| Probe Name | Detection Target | Excitation/Emission Wavelength | Application Scenarios |
|---|---|---|---|
| JC-1 | Mitochondrial Membrane Potential | 545 nm / 590 nm | Cell apoptosis, energy metabolism research |
| DiBAC4(3) | Cell Membrane Potential | 488 nm / 515 nm | Neuronal activity, cell stress |
| VSD (e.g., VF2.1.CI) | Dynamic monitoring of membrane potential | 488 nm / 515 nm | Neuronal action potentials, cellular signal transduction |
Fluorescence membrane potential detection technology is commonly used in ion channel function studies and drug screening.
| Application Areas | Description |
|---|---|
| Ion Channel Function Screening | Rapid screening of compounds related to various ion channels such as sodium, potassium, and calcium |
| Drug Safety Evaluation | Assessing the impact of drugs on critical cardiac channels such as hERG to prevent cardiac toxicity |
| Neuronal and Cardiomyocyte Function Research | Dynamic monitoring of electrical activity and signal transduction in excitable cells |
| High-Throughput Compound Library Screening | Supporting primary screening of millions of compounds to enhance new drug discovery efficiency |
| Multi-target Ion Channel Research | Compatible with multiple channel types, suitable for analyzing complex pharmacological mechanisms |
Creative Biolabs aim to accelerate your research and drug discovery in neurodegenerative diseases.
Broad Coverage of Ion Channel Targets Supported by Creative Biolabs
Creative Biolabs is equipped to screen a wide range of ion channels, including voltage-gated ion channels (such as sodium, potassium, calcium channels), ligand-gated ion channels (like GABA, NMDA, and AMPA receptors), and other ionotropic receptors.
| Ion Channel Category | Representative Subtypes | Functional Characteristics | Main Application Areas |
|---|---|---|---|
| Sodium Channels (Na+) | Nav1.1–Nav1.9, Nax | Voltage-gated, mediates action potentials | Neuropathic pain, epilepsy, arrhythmia |
| Potassium Channels (K+) | Kv11.1, Kv7.1 TWIK-1/2, Kir1.1, Kir2.x, Kir3.x, Kir6.x, etc. | Maintains resting membrane potential, regulates action potential duration | Antiepileptic, antihypertensive, arrhythmia, and safety screening |
| Calcium Channels (Ca2+) | Cav1.x, Cav2.x, Cav3.x, etc. | Mediate calcium ion influx, signal transduction | Cardiovascular diseases, neurodegenerative diseases, analgesia |
| TRP Channels | TRPV1, TRPM1, etc. | Non-selective cation channels, perceive temperature and chemical stimuli | Pain, inflammation, tumors |
| Ligand-Gated Channels | GABAAR, NMDA, nAChR, etc. | Activated by neurotransmitters, regulating neural signals | Epilepsy, anxiety, depression |
| Cyclic Nucleotide-Gated Channels (CNG) | CNGA1-4, CNGB1, CNGB3, etc. | Activated by cAMP or cGMP | Retinal diseases, olfactory disorders |
| ATP-Gated Channels (P2X) | P2X1–P2X7 | Activated by ATP, regulating immune inflammation | Inflammation, autoimmune diseases |
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Service Workflow
We have an optimized and efficient workflow, ensuring high quality at each step of the process. We also pay great attention to time efficiency and accuracy, and provide you with professional assistance during each stage, from sample testing to project delivery, to ensure your research runs smoothly.
This standardized and meticulous process ensures the reliability and scientific rigor of our service and frees you to focus on your research, while we take care of all the technical details.
Applications of Ion Channel Screening
Drug Discovery Research
Creative Biolabs employs high-throughput patch clamp, electrophysiology, and fluorescence imaging techniques to rapidly screen and optimize candidate drugs targeting different ion channels, and provide support for drug development teams to discover and develop new drugs for the treatment of neurological diseases, cardiovascular diseases, pain, and tumors.
Disease Mechanism Research
Ion channels are the key molecules in the occurrence and development of neurological, cardiovascular, immune, and metabolic diseases. Creative Biolabs offers different detection methods to help researchers discover the molecular mechanism of pathological process in neurodegenerative diseases, epilepsy, arrhythmia, autoimmune diseases and other diseases by detecting the abnormality of ion channel function and promote the development of diagnostic and therapeutic strategies.
Drug Safety Assessment
Creative Biolabs provides a professional electrophysiological testing platform to detect the toxicity risk of candidate drugs at an early stage to avoid potential safety problems and ensure the clinical safety of new drugs. Creative Biolabs integrates the membrane potential and calcium flux fluorescent probe technology to assess the impact of drugs on cell energy metabolism and apoptosis, and provide support for cell toxicity and drug safety research.
Cell Function and Signal Transduction Research
Creative Biolabs provides membrane potential fluorescent probes and calcium indicators to help researchers monitor the electrical activity and calcium signal dynamics of excitable cells such as neurons and cardiomyocytes in real-time, and promote the study of intercellular communication and signal transduction mechanisms.
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Publications
TREK-1 and TREK-2 are ubiquitously expressed in the central nervous system and periphery of mammals. The activation of TREK-1, TREK-2, or both channels might be of potential therapeutic benefit for a number of conditions including pain, migraine, ischemia, and arrhythmia. Our work focuses on identifying and optimizing novel activators for these channels.
"Selective small-molecule activators of TREK-1, TREK-2, or dual TREK-1/2 channels may present a new therapeutic opportunity for the treatment of pain."
Figure 2 TREK channels are key regulators of body temperature and ambient temperature sensing, especially
in the nervous system.3,5
Lola Rueda-Ruzafa et al. emphasized the role of TREK channels as a key regulator of body temperature and ambient temperature sensing, especially in the nervous system, to achieve the conduction and regulation of temperature sensation by regulating neuronal excitability, providing an important perspective for understanding pain and body temperature regulation mechanisms.
Kentaro Yashiro, et al. have undertaken the first step of a medicinal chemistry program on the K2P potassium ion channel family, including chemical optimization and characterization of a series of novel TWIK-related K+ channel (TREK)-1/2 dual activators and TREK-2 preferential activators, all based on hits from high-throughput screening campaigns, to provide TREK activators with good central nervous system (CNS) penetration and others with low CNS exposure to help dissect central and peripheral TREK activation. In this study, the authors have identified and optimized a series of TREK-1/2 dual activators and TREK-2 selective activators from high-throughput screens, which possess good CNS permeability, providing tool compounds for in vivo studies.
FAQs
What types of assay formats are available for ion channel screening?
Ion channel screening services typically use two main assay formats:
(1) electrophysiological assays, such as patch clamp (manual or automated) to measure ionic currents directly
(2) fluorescence-based assays to measure membrane potential or intracellular ion concentrations indirectly.
The specific protocols can be customized based on throughput and information content requirements.
How do you ensure functional expression of ion channels in cell-based assays?
We use optimized expression systems such as native cells, stably or transiently transfected cell lines, or iPSC-derived cells with attention to subunit composition and post-translational modifications since many ion channels require certain subunits, domains or cofactors for proper functional expression.
What is the throughput of the screening system?
Our platforms support high-throughput screening of millions of compounds. This can greatly speed up hit identification and optimization in drug discovery projects.
Can the screening service be customized?
Yes. We customize protocols to suit client needs, including ion channel selection, compound dosing, and data output formats to fit specific research needs and regulatory standards.
How is data quality and reproducibility maintained?
We adhere to stringent quality control protocols, including standard operating procedures, use of positive and negative controls, and statistical measures to validate assay robustness and reproducibility throughout the screening process.
How soon are results delivered?
Turnaround time depends on assay complexity and sample amount, but our streamlined workflow and automation will enable fast and reliable data delivery. Specific timelines will be determined when the project begins.
How do I initiate a screening project or request more information?
Contact us through our online inquiry form or by email. Our scientists will be glad to offer free consultation to understand your needs and provide customized solutions.
References
- Faria, R. X., L. G. B. Ferreira, and L. A. Alves. "The Mystery of P2X7 Ionotropic Receptor: From a Small Conductance Channel to a Large Conductance Channel." Neuroscience - Dealing With Frontiers, 2012. https://doi.org/10.5772/29146.
- Yashiro, Kentaro, et al. "Discovery of ONO-2920632 (VU6011887): A Highly Selective and CNS Penetrant TREK-2 (TWIK-Related K+ Channel 2) Preferring Activator In Vivo Tool Compound." ACS Chemical Neuroscience, vol. 16, no. 5, Mar. 2025, pp. 960–67. https://doi.org/10.1021/acschemneuro.5c00032.
- Rueda-Ruzafa, Lola, et al. "Are TREK Channels Temperature Sensors?" Frontiers in Cellular Neuroscience, vol. 15, Oct. 2021. https://doi.org/10.3389/fncel.2021.744702.
- Distributed under Open Access license CC BY 3.0, without modification.
- Distributed under Open Access license CC BY 4.0, without modification.
Created July 2025