TRPA1 as a therapeutic target
Transient Receptor Potential Ankyrin 1 (TRPA1) receptors are key molecular targets for the development of novel analgesics. These receptors are non-selective cation channels that are prominently expressed in nociceptors (sensory neurons) where they function as detectors for harmful environmental stimuli, tissue damage, and cellular stress. The channel is activated by a wide array of electrophilic compounds and natural irritants, including allyl isothiocyanate (AITC) from mustard oil, carvacrol, cinnamaldehyde from cinnamon, and allicin from garlic. The potential therapeutic applications of TRPA1 antagonists include, neuropathic pain, inflammatory pain and cold hypersensitivity.
TRPA1 channels rapidly desensitize which conventionally leads to a significant reduction in influx of cations (calcium/sodium) and complicates the determination of drug potencies. ChanPharm’s ion channel specialists have, therefore, developed an unique patch clamp assay for TRPA1 receptors that minimizes desensitization and ensures stable baseline conditions.
After activation by a stimulus, TRPA1 channels rapidly desensitize. This leads to a significant loss of signal (reduction in calcium/sodium influx) during repeated applications of agonists, complicating cumulative dose-response curves and antagonist screening.
Tool Compounds
The pharmaceutical industry has developed numerous antagonists to probe TRPA1 function and evaluate its clinical potential. Below is a selection of key reference and clinical compounds:
ChanPharm's TRPA1 Assays
To overcome the rapid loss of signal, ChanPharm has developed a unique patch clamp assay for TRPA1 receptors that prevents desensitization and ensures stable baseline conditions for accurate pharmacology. Furthermore, we provide validation of drug effects directly on human stem cell-derived neurons.
Screening Platforms & Technologies
SyncroPatch 384
Ion channel screening at scale.
The SyncroPatch 384 is a high-throughput automated patch clamp platform optimized for large-scale ion channel screening. It enables parallel recordings from hundreds of cells, allowing rapid assessment of compound potency, activity, and selectivity across ion channel targets.
Best suited for: Primary screening, hit confirmation, potency ranking, early off-target assessment
NANION TECHNOLOGIES HIGH THROUGHPUT
Patchliner
High-quality functional profiling with automation.
The Patchliner provides medium-throughput automated patch clamp recordings with excellent gigaseal quality and high data fidelity.
Best suited for: Secondary screening, lead optimization, mechanism-of-action studies
NANION TECHNOLOGIES MEDIUM THROUGHPUT
Manual Patch Clamp
Gold-standard ion channel electrophysiology.
Manual patch clamp provides unmatched experimental control and resolution for studying ion channel function. This is critical for TRPA1 to carefully manage desensitization states.
Best suited for: Detailed kinetics, complex protocols, validation of screening results
CONVENTIONAL SYSTEMS GOLD STANDARD