Target intelligence / Profile preview

P2X Purinergic Receptor (P2XR)

Target
P2XR
Molecular classification
Ligand-gated ion channel, Receptor
01

Overview

The P2X purinergic receptor family comprises trimeric ligand-gated ion channels activated exclusively by extracellular ATP, mediating fast excitatory responses across many tissues. Their broad distribution underlies their involvement in neurotransmission, nociception/pain pathways—including neuropathic/inflammatory conditions—immune responses via inflammasome activation (notably through subtype-specific effects like those mediated by P2RX7), vascular tone regulation, platelet function modulation—and they represent promising therapeutic targets for several major disease areas due to their unique pharmacology and pathophysiological roles.

Other names
P2X receptorATP-gated ion channel
02

Mechanism of action

Antagonism of P2X receptor subtypes, Allosteric modulation

03

Biological functions

Synaptic transmissionNociceptionInflammation regulationApoptosisSmooth muscle contractionPlatelet aggregationImmune response
04

Disease associations

Chronic inflammationNeuropathic painInflammatory painCancer progressionNeurodegenerative disordersCardiovascular diseaseEndocrine dysfunctions
05

Safety considerations

Potential for off-target effects due to widespread expressionSubtype selectivity challenges
06

Interacting drugs

A317491

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