P2X purinoceptor family (P2XR) (P2XR)

The P2X purinoceptor family consists of seven distinct subunits (P2X1–P2X7) that assemble into homo- or heterotrimeric ligand-gated ion channels (IUPHAR/BPS Guide to Pharmacology). These receptors are primarily activated by extracellular adenosine triphosphate (ATP), leading to the influx of cations such as sodium, potassium, and calcium (UniProt). They play critical roles in diverse physiological processes, including fast excitatory neurotransmission, smooth muscle contraction, and the modulation of inflammatory responses through the NLRP3 inflammasome (Burnstock, 2017, PubMed). In pathological states, overactivation of P2X receptors is linked to chronic pain, respiratory conditions like chronic cough, and various inflammatory diseases (Nature Reviews Drug Discovery, 2021). Therapeutic strategies often focus on subtype-specific antagonists, such as P2X3 inhibitors for cough or P2X7 inhibitors for neuroinflammation, though achieving selectivity remains a challenge to avoid side effects like taste impairment (StatPearls).

Other names

P2X receptorsATP-gated ion channelsPurinergic P2X receptorsIonotropic purinergic receptorsP2X family purinoceptors

Antagonism of ATP-gated ion channels to inhibit cation influx and downstream signaling pathways, such as the release of pro-inflammatory cytokines or neuronal depolarization (IUPHAR/BPS).