ATP-gated P2X receptor cation channel family , or simply P2X receptor family, consists of cation-permeable ligand-gated ion channels that open in response to the binding of extracellular adenosine 5'-triphosphate. They belong to a larger family of receptors known as the ENaC/P2X superfamily. ENaC and P2X receptors have similar 3-D structures and are homologous. P2X receptors are present in multiple organisms including humans, mouse, rat, rabbit, chicken, zebrafish, bullfrog, fluke, and amoeba.

There are 7 known P2X subunits

• P2X1

• P2X2

• P2X3

• P2X4

• P2X5

• P2X6

• P2X7

P2X receptors are known as the purinergic receptors and have been indicated to play a role nociception, inflammation and airway hyperactivity.

Fig. 1 Antagonism of P2X receptor-mediated currents in rat mesenteric artery smooth muscle cells

Here in Creative Bioarray, we provide target screening on a series of P2X channels listed as below:

P2X1 (P2RX1)

Tissue-specific Location: smooth muscle, platelets and sensory neurons.

Disease: P2RX1 mutation has been linked to a severe bleeding disorder arising from impaired ADP-induced platelet aggregation.

Therapeutic Targets: urinary incontinence and pain.

P2X4 (P2RX4)

Tissue-specific Location: CNS, alveolar macrophages, vascular endothelium and airway smooth muscle.

Therapeutic Trgets: neuropathic pain, asthma and heart failure.

P2X7 (P2RX7)

Tissue-specific location: lymphocytes and microglia.

Therapeutic targets: osteoporosis, neuropathic and inflammatory pain and also immune diseases.

Reference

1. Lewis CJ, Evans RJ. Lack of run-down of smooth muscle P2X receptor currents recorded with the amphotericin permeabilized patch technique, physiological and pharmacological characterization of the properties of mesenteric artery P2X receptor ion channels. Br J Pharmacol. 2000; 131: 1659–1666.

Related Section

• Sodium Channels
• Calcium Channels
• Potassium Channels
• Chloride Channels
• TRP Channels
• ASICs
• Nicotinic Acetylcholine Receptors
• Ionotropic Glutamate-gated Receptors
• GABAa Receptors
• Glycine Receptors
• 5-HT Receptors3
• Cystic Fibrosis Transmembrane Conductance Regulators (CFTR)
• Other Ion Channels