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P2X receptor antagonists and modulators act on ion channels gated by extracellular adenosine triphosphate (ATP). Cloning of the P2X1 and P2X2 subunits in 1994 defined a new structural class of ligand-gated ion channels. Seven subunits, P2X1 to P2X7, assemble as trimers that pass sodium, potassium and calcium ions. P2X3 and P2X2/3 receptors on sensory neurons are studied in pain signaling, and P2X7 receptors in inflammation. In 1996 the cytolytic P2Z receptor of macrophages was identified as P2X7, which opens large pores during sustained ATP exposure. A-317491 sodium salt hydrate and AF-353 block P2X3 and P2X2/3 receptors. A 740003 and A 438079 hydrochloride are P2X7 antagonists, whereas NF 279 acts at P2X1.
Synonyms: GW-791343
GW791343 HCl acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2) and a positive allosteric modulator of rat P2X7.
Synonyms: GW 791343
GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
GSK-1482160 is a negative allosteric modulator of the P2X7 receptor (P2X7R), with high oral bioavailability and the ability to penetrate the blood-brain barrier. It has demonstrated a human pIC50 of 8.5 and a rat pIC50 of 6.5, effectively reducing ATP's efficacy at the receptor without altering its affinity, which subsequently inhibits IL-1β release. This compound serves as a valuable radioligand for P2X7R imaging using isotopes such as 11C or 18F and is applicable in research related to chronic joint pain and chronic constriction injury (CCI).
P2X2/3 modulator-1 is a selective modulator targeting the P2X2 and P2X3 purinergic receptors. This compound exhibits significant biological activity in the modulation of pain pathways and inflammation processes. It is applicable in research focused on pain management, central nervous system disorders, and inflammatory conditions, providing insights into therapeutic strategies for these ailments.
P2X7 receptor antagonist-6 is a negative allosteric modulator targeting the P2X7 receptor, exhibiting an IC50 of 1.31 μM for human P2X7. This compound demonstrates potential for research applications in cancer, neurodegenerative disorders, inflammatory responses, and infectious diseases, contributing to a greater understanding of P2X7's role in these conditions. Its specificity and efficacy make it a valuable tool for exploring therapeutic pathways in related research fields.
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GSK-1482160 isomer functions as a negative allosteric modulator of the P2X7 receptor (P2X7R), exhibiting oral bioavailability and the ability to penetrate the blood-brain barrier. With pIC50 values of 8.5 for human and 6.5 for rat, this compound effectively diminishes ATP's efficacy at P2X7R without altering its affinity, thus inhibiting the release of IL-1β. Additionally, GSK-1482160 serves as an excellent radioligand, available for labeling with isotopes such as 11C or 18F for imaging studies. Its applications extend to the investigation of chronic joint pain and the chronic constriction injury (CCI) model.
