Target intelligence / Profile preview

Transient receptor potential cation channel subfamily C member 4 (TRPC4) (TRPC4)

Target
TRPC4
Molecular classification
Ion channel, Transient receptor potential channel, Non-selective cation channel
01

Overview

Transient receptor potential cation channel subfamily C member 4 (TRPC4) is a non-selective cation channel that plays a critical role in regulating intracellular calcium levels and membrane potential (UniProt: Q9UBN4). It is widely expressed in the central nervous system, particularly in the amygdala and hippocampus, as well as in smooth muscle and endothelial cells (PubMed: 19448621). TRPC4 is activated downstream of G protein-coupled receptors (GPCRs) that stimulate the phospholipase C (PLC) pathway. In the brain, TRPC4 is implicated in the modulation of anxiety and fear-related behaviors, making it a target for neuropsychiatric disorders (PubMed: 25339648). In the periphery, it contributes to smooth muscle contraction and vascular permeability, suggesting roles in gastrointestinal and cardiovascular diseases. Pharmacological inhibition of TRPC4, often in conjunction with TRPC5, is being explored for treating anxiety, depression, and certain types of chronic pain (PubChem: ML204).

Other names
TRP4CCE1HTRP4Trp-related protein 4Transient receptor potential channel 4
02

Mechanism of action

Inhibition of non-selective cation influx and modulation of intracellular calcium signaling (PubMed: 21233414)

03

Biological functions

Calcium signalingSignal transductionSmooth muscle contractionNeurotransmissionVasodilationEndothelial permeability
04

Disease associations

AnxietyDepressionGastrointestinal disorderCardiovascular diseaseRenal cell carcinomaChronic pain
05

Safety considerations

Off-target effects on TRPC5Potential CNS side effectsCardiovascular regulation issues
06

Interacting drugs

ML204

3 more in the full profile.

07

Biomarkers

TRPC4 protein expressionTRPC4 mRNA levelsIntracellular calcium flux

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