Webinar Recap: Ion Channel Drug Discovery – Recent Advances in Novel Non-Opioid Pain Research

Ion Channel Product Solutions

 
Ion channels represent a key target class for therapeutics to treat human disease. The prevalence of debilitating pain disorders and opioid misuse has led to the need for developing new non-addictive molecules.
 
Voltage-gated sodium channels (Nav’s) are responsible for transmitting pain signals, of which Nav1.8, found in peripheral nociceptors, is a validated target for pain treatment. The development of an effective inhibitor of Nav1.8 ion channels can reduce the transmission of pain signals from the dorsal root ganglion (DRG) neurons to the brain and can lead to an effective analgesic. Opioid drugs act by depressing neuronal excitability by reducing the activity of Ca2+ channels and increasing the activity of K+ channels in the pain pathway, whereas direct inhibition of Nav1.8 ion channels presents an attractive non-addictive alternative for developing analgesics.
 
On May 15, 2024, Dr. John Gilchrist of Latigo Biotherapeutics and Dr. James Costantin of Eurofins DiscoverX® presented a webinar outlining recent advances in non-opioid pain research.
 
Dr. Gilchrist presented results from a recently published work describing the potency, pharmacology, interaction site, and mechanism of action (MOA) of LTGO-33, a novel, potent, and selective Nav1.8 inhibitor developed by Latigo Biotherapeutics. The study used PrecisION™ stable cell lines expressing human and rat Nav1.8 channels from Eurofins DiscoverX and demonstrated the suitability of these cell lines for drug discovery and development.
 
Please refer to this publication for more information about the study,
Gilchrist JM, Yang ND, Jiang V, Moyer BD. Pharmacologic Characterization of LTGO-33, a Selective Small Molecule Inhibitor of the Voltage-Gated Sodium Channel NaV1.8 with a Unique Mechanism of Action. Mol Pharmacol. 2024 Feb 15;105(3):233-249. doi: 10.1124/molpharm.123.000789. PMID: 38195157.
 
For on-demand access to a webinar on the subject, Ion Channel Webinar
 
Further, data was presented by Dr. Costantin introducing cardiac safety targets in a frozen ready-to-assay cell format to support ion channel drug discovery programs.

Ion Channel Product Solutions

Eurofins DiscoverX’s comprehensive portfolio of functionally validated ion channel products is comprised of optimized and validated PrecisION stable ion-channel cell lines for use in cell-based assays, PathHunter® pharmacotrafficking assays for pharmacochaperone discovery, and a hERG ion channel membrane prep for safety and binding studies.
 
The vast ion channel product solutions allow assessment of voltage-gated, ligand-gated, as well as other ion channel targets for your drug discovery and safety applications. The ion channel cell lines are pharmacologically and functionally validated using in-house discovery and safety services laboratories. Their biophysical and pharmacological properties are characterized electrophysiologically using conventional manual patch-clamp and multiple automated patch-clamp platforms by experienced electrophysiologists in both Eurofins Discovery services and Eurofins DiscoverX products laboratories.
 
 

Author

Arvind Kannan
 
Arvind Kannan is a Marketing Manager at Eurofins DiscoverX. He holds a Ph.D. in Cell & Molecular Biology with a focus on anti-cancer peptides from the University of Arkansas. His M.S degree is from Birla Institute of Technology & Science in Medical lab technology, while Bachelors’ in Biochemistry is from the University of Madras, India