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Target intelligence / Profile preview
Transient Receptor Potential Melastatin Subfamily Member 8 (TRPM8)
- Target
- TRPM8
- Molecular classification
- Ion channel, TRP channel, Receptor, Voltage-gated ion channel
01
Overview
Transient receptor potential melastatin subfamily 8 (TRPM8) is a non-selective, voltage-gated cation channel that acts as the primary molecular sensor for environmental cold and cooling agents like menthol. It is highly expressed in sensory neurons and plays a crucial role in cold sensation, thermoregulation, and pain modulation. Dysregulation of TRPM8 has been implicated in various diseases, including neuropathic pain, migraine, bladder disorders, dry eye syndrome, and certain cancers, making it a potential therapeutic target.
- Other names
- Cold and menthol-sensitive receptor 1 (CMR1)TRP-p8
02
Mechanism of action
Agonists bind to TRPM8, opening the channel and allowing influx of Na+ and Ca2+, leading to cellular depolarization and action potential generation. Antagonists block the channel, preventing ion influx and reducing neuronal excitability.
03
Biological functions
Cold sensation/transductionThermoregulationPain perception modulationCalcium signalingRegulation of neuronal excitability
04
Disease associations
Neuropathic painCold allodyniaMigraineOveractive/painful bladder syndromesDry eye syndromeProstate cancerPancreatic cancerColon cancerBreast cancerLung cancer
05
Safety considerations
Specificity challenges for TRPM8 antagonistsPotential for off-target effectsCalcium-dependent desensitization during sustained stimulation
06
Interacting drugs
Menthol
4 more in the full profile.
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