Enhancing the Efficiency of TRP Channel Drug Discovery

Transient receptor potential (TRP) channels constitute a class of ion channels widely distributed across various tissues, particularly in the peripheral and central nervous systems. These channels respond to diverse intracellular and extracellular stimuli, participating in various physiological pathways. For example, TRPV1 can be activated by capsaicin and acidic conditions, while the TRPA1 channel responds to cold stimuli and compounds like AITC. Moreover, TRP ion channels serve as critical therapeutic targets for inflammation, cancer, and other diseases.

The FLIPR platform delivers exceptional luminescence performance and facilitates high-quality data acquisition with the assistance of a mechanical arm. It monitors calcium flux, potassium flux, and membrane potential, commonly used for GPCR and ion channel targets.

In our TRP family assays, based on FLIPR, we’ve successfully established stable cell lines expressing TRPV1, TRPV4, TRPA1, TRPC5, TRPC6, TRPM8, and TRPML1. These cell lines provide robust support for subsequent calcium flux assays and membrane potential measurements, overcoming challenges in ion channel drug discovery.

Our assays provide reliable results, ensuring consistent repeatability across multiple trials. This convenience makes them ideal tools for screening compounds targeting the TRP ion channels. Below, you’ll find figures presenting our data on the TRPV1, TRPC6, and TRPML1 targets.