P2X7 Receptor
P2X7 receptor (P2X7R) is a trimeric ATP-gated cation channel expressed predominantly, but not exclusively, on immune cells[1]. Mechanistically, extracellular ATP at tissue injury and inflammation sites activates P2X7R, linking purinergic signaling to NLRP3 inflammasome activation, cytokine and chemokine release, transcription factor activation, and cell death[2]. P2X7R activation induces NLRP3 inflammasome formation and inflammatory caspase-1 activation, which drives pyroptosis and release of pro-inflammatory cytokines[3]. In disease models, P2X7 antagonists have been used in rodent studies of neurologic disease, injury, inflammation, and musculoskeletal disorders[1]. Compared with related P2X receptors, P2X7R shows distinctive splice complexity, with ten human P2RX7 splice variants and several SNP-defined haplotypes reported[2]. Structural studies further support subtype-specific antagonist design because mammalian P2X7R structures complexed with five unrelated antagonists revealed a shared allosteric inhibition mechanism[4]. Therefore, P2X7R agonists and inhibitors provide practical tools for studying ATP-driven inflammation, inflammasome signaling, immune-cell activation, and disease-relevant receptor pharmacology[1][2][3][4].
Verweise:
- [1]. Bartlett R, et al. The P2X7 receptor channel: recent developments and the use of P2X7 antagonists in models of disease. Pharmacol Rev. 2014 Jul;66(3):638-75. [Content Brief]
- [2]. Di Virgilio F, et al. The P2X7 Receptor in Infection and Inflammation. Immunity. 2017 Jul 18;47(1):15-31. [Content Brief]
- [3]. Pelegrin P. P2X7 receptor and the NLRP3 inflammasome: Partners in crime. Biochem Pharmacol. 2021 May;187:114385. doi: 10.1016/j.bcp.2020.114385. Epub 2020 Dec 20. PMID: 33359010. et al. P2X7 receptor and the NLRP3 inflammasome: Partners in crime. Biochem Pharmacol. 2021 May;187:114385. [Content Brief]
- [4]. Karasawa A, et al. Structural basis for subtype-specific inhibition of the P2X7 receptor. Elife. 2016 Dec 9;5:e22153. [Content Brief]
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P2X7 Receptor Verwandte Produkte (32)
Verwandte Produkte (32)
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A 839977
0 ImagesA 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.
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Zeaxanthin dipalmitate
0 ImagesZeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1 (AdipoR1; Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP).
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Lu AF27139
0 ImagesLu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases.
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GW791343 dihydrochloride
0 ImagesGW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease.
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(S)-JNJ-54166060
0 ImagesArt. -Nr.: HY-124300ACAS. Nr.: 1627900-42-8(S)-JNJ-54166060 is an enantiomer of JNJ 54166060. JNJ 54166060 is a potent P2X7 antagonist.
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EVT-401
0 ImagesArt. -Nr.: HY-178230CAS. Nr.: 951015-69-3EVT-401 is an orally active, potent and highly selective human P2X7R antagonist, with an IC50 of 10 nM and a Ki of 7.6 nM for human P2X7R, and an IC50 of 220 nM for mouse P2X7R. EVT-401 promotes apoptosis and induces cell cycle arrest in human rheumatoid arthritis synovial fibroblasts (RA SF), reduces the production of proinflammatory and joint-destructive mediators, and mitigates aggressive phenotypes. EVT-401 exhibits favorable oral bioavailability and a good safety profile, making it suitable for research into rheumatoid arthritis.
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P2X7 receptor antagonist-3
0 ImagesArt. -Nr.: HY-148558CAS. Nr.: 1627900-92-8P2X7 receptor antagonist-3 is a potent P2X7 receptor antagonist with P2X7R IC50 values of 4.2 nM in humans and 6.8 nM in rats.
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UB-MBX-46
0 ImagesArt. -Nr.: HY-179373UB-MBX-46 is a potent and selective P2X7 receptor antagonist with IC50s of 0.514 nM (hP2X7R), 40.6 nM (rP2X7R), and 4.52 nM (mP2X7R), respectively. UB-MBX-46 interacts with the classical allosteric pocket of the human P2X7 receptor. UB-MBX-46 can be used for cancer, atherosclerosis, and neurode generation research.
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P2X7 receptor antagonist-6
0 ImagesArt. -Nr.: HY-175196CAS. Nr.: 1114621-31-6P2X7 receptor antagonist-6 (Compound 2g) is a negative allosteric P2X7 receptor antagonist with an IC50 of 1.31 μM for hP2X7. P2X7 receptor antagonist-6 can be used for cancer, neurodegenerative, inflammatory, and infectious diseases research.
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α,β-Methylene-ATP dilithium
0 ImagesArt. -Nr.: HY-134440CAS. Nr.: 104809-20-3α,β-Methylene-ATP dilithium is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP dilithium can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP dilithium also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP dilithium can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system.
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GW791343 trihydrochloride
0 ImagesArt. -Nr.: HY-15470CAS. Nr.: 309712-55-8GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease.
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