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Last update 31 Jan 2026
P2X7 receptor antagonists(Chengdu University)
Last update 31 Jan 2026
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms Compound 13a(Chengdu University) |
Target |
Action antagonists |
Mechanism P2X7 receptor antagonists(P2X purinoceptor 7 antagonists) |
Therapeutic Areas |
Active Indication |
Inactive Indication- |
Originator Organization |
Active Organization |
Inactive Organization- |
License Organization- |
Drug Highest PhasePreclinical |
First Approval Date- |
Regulation- |
Structure/Sequence
Molecular FormulaC21H17F3N6O3S2 |
InChIKeyJRMLTYBLQKCPLC-GFCCVEGCSA-N |
CAS Registry3046388-17-1 |
Related
100 Clinical Results associated with P2X7 receptor antagonists(Chengdu University)
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100 Translational Medicine associated with P2X7 receptor antagonists(Chengdu University)
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100 Patents (Medical) associated with P2X7 receptor antagonists(Chengdu University)
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71
Literatures (Medical) associated with P2X7 receptor antagonists(Chengdu University)01 Feb 2026NEUROSCIENCE
Antidepressants as modulators of P2X7 receptor activity
Review
Author: Vidal, Vitor Nascimento ; Teixeira, Guilherme Pegas ; Faria, Robson Xavier ; de Souza Oliveira, Jonathas Albertino ; Faria, Juliana Vieira ; Rocha, Leandro ; Bello, Murilo Lamim
According to the Pan American Health Organization, more than 300 million people suffer from depression worldwide. Despite the alarming numbers, current drug treatments produce partial results, as they focus on only one pillar of depression: neurotransmitters. Most current medications for depression focus only on stimulating increased levels of neurotransmitters related to feelings of well-being and happiness, such as serotonin and norepinephrine, which, despite providing relief, do not produce such impressive results for patients. A significant and scientifically endorsed point regarding depression is neuroinflammation. The relationship between inflammation in the body and the development or worsening of depression has been strongly reinforced by neuroscientific studies. Studies have also shown that depressed patients have increased levels of inflammatory cytokines. Antidepressants have already demonstrated anti-inflammatory activity, stimulating the production of anti-inflammatory cytokines and reducing the production of oxidative radicals, as in the case of fluoxetine and paroxetine. In depression, P2X7 receptor expression is increased. This receptor is activated, and greater expression produces a depressive phenotype, while its blockade has antidepressant effects. Therefore, we evaluated the in-silico interaction between antidepressants and the allosteric site of the P2X7 receptor. This finding reinforces the functional data in the literature that point to the inhibition of the P2X7 receptor. The molecular docking results showed that drugs containing the amino acids TYR295 and PHE95 are essential for a good interaction with the P2X7 receptor at its allosteric site. Furthermore, this study demonstrated that combining antidepressants with p2x7 receptor antagonists can attenuate neuroinflammation.
01 Jan 2026British Journal of Pharmacology
P2X7 receptor antagonism suppresses epileptiform‐like activity in an inflammation‐primed human iPSC‐derived neuron model of drug‐resistant epilepsy
Article
Author: Prehn, Jochen H. M. ; Kesavan, Jaideep ; Wang, Yitao ; Engel, Tobias ; Dinkel, Klaus ; Henshall, David C. ; Hamacher, Michael
Background and Purpose:
Neuroinflammation is increasingly recognised to contribute to drug‐resistant epilepsy. Activation of ATP‐gated P2X7 receptors has emerged as an important upstream mechanism, and increased P2X7 receptor expression is present in the seizure focus in rodent models and patients. Pharmacological antagonists of P2X7 receptors attenuate seizures in rodents, but this has not been explored in human neural networks.
Experimental Approach:
Human neurons were differentiated from two human induced pluripotent stem cell (hiPSC) lines. P2X7 receptor function on neurons was assessed via the calcium transients evoked by the agonist BzATP. Acute or chronic models of epileptiform‐like events were generated by exposing hiPSC cultures to the GABA
A
receptor antagonist picrotoxin or a cocktail of picrotoxin and neuroinflammatory agents, with or without P2X7 receptor antagonists. Epileptiform‐like activity was measured via single cell patch‐clamp recordings.
Key Results:
BzATP application (300 μM) resulted in increased calcium influx in hiPSC‐derived neurons which was blocked by the P2X7 receptor antagonists JNJ‐47965567 (100 nM) and AFC‐5128 (30 nM). Single‐cell patch‐clamp recordings showed that, while treatment with AFC‐5128 did not reduce epileptiform‐like activity triggered by picrotoxin alone, AFC‐5128 reduced the severity of epileptiform‐like activity under inflammatory conditions. Notably, epileptiform‐like events in the inflammation‐primed picrotoxin model were refractory to the anti‐seizure medication carbamazepine alone but were reduced by the co‐application of carbamazepine with AFC‐5128.
Conclusions and Implications:
Our findings demonstrate anti‐seizure effects of targeting P2X7 receptors in a human neuronal network model of epilepsy and suggest P2X7 receptor‐based treatments may be effective add‐on treatments for controlling drug‐resistant seizures.
01 Dec 2025Purinergic Signalling
The P2X7 receptor in leukemia: pathological mechanisms and therapeutic potential
Review
Author: Peng, Xiaoxiang ; Zhao, Ronglan ; Xue, Yanwen ; Yan, Meng ; Cao, Yahui ; Du, Yanan
The P2X7 receptor is a trimeric ion channel purinergic receptor. It plays a crucial part in the pathophysiology of cancers and a variety of inflammatory diseases and is widely expressed in different cell types. Leukemia represents a type of malignant clonal disorder that impacts the hematopoietic stem cells. Chemotherapy is one of the main treatment methods for leukemia, but there are also many side effects. In recent years, targeted therapy is a new treatment method. Research has shown that the progression and occurrence of leukemia is significantly related to the P2X7 receptor. The P2X7 receptor is also involved in the migration and invasion of leukemia cells. Furthermore, the polymorphism of the P2X7 receptor gene also takes on a significant function in the occurrence, development and clinical course of leukemia patients. The P2X7 receptor inhibitors have been found to work better in combination with existing therapeutics. Therefore, the P2X7 receptor may serve as a potential therapeutic target.
1
News (Medical) associated with P2X7 receptor antagonists(Chengdu University)
100 Deals associated with P2X7 receptor antagonists(Chengdu University)
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R&D Status
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Chronic Kidney Diseases | Preclinical | China | 23 Sep 2024 |
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