Ion Channel Screening Services

Overview of Ion Channel Screening in Neuroscience Research

Ion channels are important pharmacological targets for drug intervention and treatment of disorders in the central nervous system (CNS). Equipped with cutting-edge technology and experts using the most up-to-date methodologies, Creative Biolabs is your ion channel screening program partner to meet all your specific requirements.

Introduction to Ion Channels as Therapeutic Targets

Ion channels regulate crucial electrical functions throughout the body, including the heartbeat, sensory transduction, and CNS function. Given the central role in many physiological processes, they represent an attractive target class for drug discovery. They are enormous potential for the intervention of disease states in various disorders, particularly in the CNS and cardiovascular systems. The recognized importance of ion channel proteins in health and disease has led to an active search for ion channel targets and novel therapeutics in the worldwide drug discovery market.

Ion Channel Screening

Ion channels underlie numerous physiological processes and present unique challenges in drug discovery screening, owing to complex multisubunit architectures and practical considerations when measuring their activity with any degree of throughput. Therefore, high-throughput ion channel screening technologies are commonly utilized for ion channel drug discovery. Recently, two major and highly complementary strategies have formed the basis for cell-based ion channel screening: the highest throughput optical assays representing indirect measures of ion channel function and the introduction of higher-throughput electrophysiological methodologies. These approaches permit an efficient and integrated process for ion channel drug discovery.

• First, non-electrophysiological approaches such as ion flux measurements directly and optical approaches to ion flux and membrane potential measurements are established and validated. Ion-flux methods have been used successfully to identify many ion channel modulators.
• Second, ion channel function can be monitored using membrane potential-sensitive fluorescent dyes in fluorescence-based assays.
• In addition, ion channel screening would be greatly facilitated by developing novel, HTS-compatible assays with improved voltage control and kinetic resolution based on electrophysiological screening technologies. The ability to study ion channels by voltage clamp and their drug interactions with enhanced throughput plays a key role in the development of novel ion channel-targeted drugs.

Services at Creative Biolabs

With increased recognition of the importance of ion channels in disease processes, the last ten years have witnessed tremendous progress in functional ion channel-screening technologies and their implementation for ion channel drug discovery. The current functional screening technologies have been advanced to a point where understanding of the biology and pathophysiological relevance of ion channels in a disease context and the design of enhanced ion channel-targeted chemical libraries become the rate-limiting factors for meaningful drug discovery. For this fast-paced area of research, Creative Biolabs provides state-of-the-art ion channel screening solutions to researchers all over the world. Our system provides a platform for fully automated high-throughput screening and pharmacological characterization of ion channel modulators. We look forward to discussing the projects and finding the best solution for your needs.

Ion channels are attractive targets for drug discovery in CNS. With our advanced platform and extensive experience, Creative Biolabs is confident in offering the best ion channel screening services, including

• Potassium Channel Screening
• Sodium Channel Screening
• Calcium Channel Screening
• Ligand-gated Channel Screening

We guarantee the results for our customers all over the world. Please do not hesitate to contact us or reach us by e-mail or phone with your particular needs.

Our ion channel screening platform utilizes advanced technologies and techniques to screen a large library of compounds for their ability to modulate specific ion channels. This screening process involves high-throughput assays that measure the activity of ion channels in response to different compounds.

• We use a variety of cell-based and biochemical assays to assess the effects of compounds on ion channel function, including voltage-gated ion channels, ligand-gated ion channels, and calcium channels.
• We can screen compounds for their ability to enhance or inhibit ion channel activity, as well as assess their selectivity and potency. Our ion channel screening in neuroscience services are suitable for a wide range of applications, including target validation, lead optimization, and safety profiling.
• Once screening is complete, we provide our clients with detailed data analysis and interpretation, as well as recommendations for further drug development.

Our goal is to help accelerate the discovery and development of novel therapeutics for neurological disorders by providing high-quality ion channel screening services in neuroscience. Our services are for research use only and are not intended for diagnostic or therapeutic purposes. By rendering this service and related services, we aim to accelerate research and drug discovery in neurodegenerative diseases, including but not limited to:

Published Data

TREK1 expression is predominantly detected in the brain, and TREK1 has also been associated with a variety of pathological conditions including, but not limited to, stroke, epilepsy, depression, or inflammation. Christina B. Schroeter, et al. performed a high-throughput screening for new TREK1 activators using improved potassium channel analysis. They attempted to identify new TREK1 channel activators and validate the regulatory potential of these substances in vitro.

They used HTS to identify and characterize new TREK1 activators, selecting FluxOR potassium channel analysis, a system suitable for detecting TREK1 potassium channel activation in HEK293T/TREK1 cells. They selected a collection of enamine compounds for screening, which included low molecular weight organic compounds as well as various drug-like compounds.

Fig. 1 FluxOR potassium ion channel assay.¹

Applications of Ion Channel Screening in Neuroscience

Our ion channel screening technology offers a variety of applications in neuroscience research.

• Electrophysiology studies - It can be used to measure the electrical activity of neurons in response to various stimuli, providing insights into the underlying mechanisms of neuronal signaling and synaptic transmission.
• Neurotoxicity testing - Our technology allows researchers to assess the effects of these compounds on ion channel activity, providing valuable information on their potential neurotoxic effects.
• Drug discovery - Our technology allows researchers to screen potential drug candidates for their ability to modulate specific ion channels, leading to the discovery of novel therapeutic agents.
• Mechanistic studies - By using our ion channel screening technology, researchers can study the biophysical properties of ion channels, such as their conductance, selectivity, and gating kinetics, to better understand how they contribute to normal brain function and dysfunction in neurological diseases.

FAQs

Q: What types of ion channels can you screen for in your facility?

A: Our facility 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. We use advanced technologies like automated patch-clamp systems and fluorescence-based assays to ensure high-throughput and precise measurements. This versatility allows us to support various research needs in neuroscience.

Q: What kind of data output can we expect from your ion channel screening service?

A: From our ion channel screening service, you can expect detailed quantitative data on ion channel activity, including current amplitudes, voltage dependencies, and kinetics. We provide comprehensive reports featuring raw data, graphical representations, statistical analyses, and interpretative summaries. Additionally, we offer data in formats compatible with various analysis software, ensuring you can seamlessly integrate our results into your ongoing research.

Q: What are the costs associated with your ion channel screening services?

A: The costs of our ion channel screening services vary depending on the scope and complexity of the project. Factors influencing the price include the number of ion channels screened, the type and number of assays performed, and any customization required. We offer competitive pricing and are happy to provide a detailed quote based on your specific needs. Please contact us directly to discuss your project and obtain a personalized estimate.

Q: What kind of experience and expertise does your team have in ion channel screening?

A: Our team consists of highly skilled scientists with extensive experience in ion channel research and screening. Many hold advanced degrees in neuroscience, pharmacology, and related fields, and have a proven track record of successful projects and publications. Our expertise spans various ion channel types and screening technologies, ensuring we can deliver high-quality, reliable data tailored to your research needs. We are committed to staying at the forefront of scientific advancements to provide you with the best possible service.

Scientific Resources

Glutamate Receptor Ion Channels: Mediating Synaptic Signaling in Neurons

Ion Channels in Neurogliomas

Reference

1. Schroeter, Christina B., et al. "Validation of TREK1 ion channel activators as an immunomodulatory and neuroprotective strategy in neuroinflammation." Biological Chemistry 404.4 (2023): 355-375.

For Research Use Only. Not For Clinical Use.