Target intelligence / Profile preview

Transient receptor potential canonical channel 5 (TRPC5)

Target
TRPC5
Molecular classification
Ion channel, Cation channel, Receptor-activated channel, Transient receptor potential channel (TRP channel), Calcium channel
01

Overview

Transient receptor potential canonical channel 5 (TRPC5) is a calcium-permeable, non-selective cation channel that forms part of the larger TRP channel superfamily. It is primarily expressed in the central nervous system but found also in peripheral tissues such as the kidney, vasculature, and sensory neurons. TRPC5 channels can form homo- or heterotetrameric complexes (with TRPC1 or TRPC4), are activated by G protein-coupled receptor signaling, membrane stretch, cold, and various intracellular and extracellular stimuli (e.g., phospholipase C, nitric oxide, lysophospholipids). The channel contributes to calcium signaling, neuronal excitability, vascular tone regulation, and sensory processes including innocuous cold sensing. TRPC5 has been implicated in several physiological and pathological processes such as anxiety, seizure susceptibility, and vascular dysfunction. Pharmacologically, the channel is targetable by anesthetics, and small-molecule inhibitors are being studied for their potential utility in neurological and cardiovascular diseases.

Other names
TRPC5Short transient receptor potential channel 5Transient receptor protein 5TRP-5
02

Mechanism of action

Modulation of calcium influx via channel inhibition or activation; Alteration of membrane excitability (by influencing Ca²⁺ and Na⁺ permeability); Receptor-operated channel gating (via G protein-coupled receptor signaling)

03

Biological functions

Calcium signalingNeurotransmissionAxon guidanceVascular smooth muscle cell migration and contractilityThermosensation (cold sensing)Electrophysiological homeostasis
04

Disease associations

Neurological disease (including anxiety, seizures, fear)Cardiovascular diseasePain and cold perception disordersPotential involvement in intellectual disabilityVascular dysfunction
05

Safety considerations

Potential for CNS side effects given CNS enrichmentUnintended cardiovascular and renal effects due to peripheral expressionPossible altered pain or temperature sensation as TRPC5 is involved in cold sensingOff-target effects if inhibitors are not selective for TRPC5 over related channels
06

Interacting drugs

Chloroform

4 more in the full profile.

07

Biomarkers

Expression levels of TRPC5 (e.g., in CNS regions, sensory neurons) may serve as biomarkers in research, especially for neurological and vascular conditionsNo established clinical biomarkers for patient selection reported in major clinical studies

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