Target intelligence / Profile preview

Transient Receptor Potential Melastatin 8 (TRPM8)

Target
TRPM8
Molecular classification
Ion channel, TRP channel, Voltage-gated ion channel
01

Overview

TRPM8 is a voltage-gated, nonselective cation channel and a member of the transient receptor potential (TRP) ion channel superfamily. It is the primary molecular sensor for environmental cold and cooling agents such as menthol. Activation leads to influx of cations, depolarization, and ultimately sensations of coolness or cold pain. It is highly expressed in sensory neurons but also found in other tissues, where its function is less well understood. TRPM8 is implicated in pain, cancer, migraine, and dry eye disease.

Other names
Transient receptor potential cation channel subfamily M member 8
02

Mechanism of action

Activation by cold or chemical agonists leads to Na+ and Ca2+ influx, cell depolarization, and action potential generation.

03

Biological functions

Sensory transductionThermoregulationDetection of cold temperaturesDetection of cooling agentsIon transport
04

Disease associations

Pain syndromesCold allodyniaCancerProstate cancerPancreatic cancerColon cancerBreast cancerMigraineDry eye disease
05

Safety considerations

Off-target effects in other tissues due to widespread expression.Potential for altered thermoregulation.Calcium-dependent desensitization affects drug efficacy.
06

Interacting drugs

Menthol

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