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Activation and regulation of purinergic P2X receptor channels

Pharmacological reviews, 2011-09, Vol.63 (3), p.641-683

2011

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Action of MK‐7264 (gefapixant) at human P2X3 and P2X2/3 receptors and in vivo efficacy in models of sensitisation

British journal of pharmacology, 2019-07, Vol.176 (13), p.2279-2291

2019

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Microglial P2X4R-evoked pain hypersensitivity is sexually dimorphic in rats

Pain (Amsterdam), 2018-09, Vol.159 (9), p.1752-1763

2018

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X-ray structures define human P2X(3) receptor gating cycle and antagonist action

Nature (London), 2016-10, Vol.538 (7623), p.66

2016

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Purinergic P2X receptors: Structural models and analysis of ligand-target interaction

European journal of medicinal chemistry, 2015-01, Vol.89, p.561-580

2015

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The P2X7 receptor channel: recent developments and the use of P2X7 antagonists in models of disease

Pharmacological reviews, 2014-07, Vol.66 (3), p.638-675

2014

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P2X7 receptor antagonism: Implications in diabetic retinopathy

Biochemical pharmacology, 2017-08, Vol.138, p.130-139

2017

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P2X7 receptor in multifaceted cellular signalling and its relevance as a potential therapeutic target in different diseases

European journal of pharmacology, 2021-09, Vol.906, p.174235-174235, Article 174235

2021

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Pharmacodynamics, pharmacokinetics and CYP3A4 interaction potential of the selective P2X3 receptor antagonist filapixant: A randomized multiple ascending‐dose study in healthy young men

British journal of clinical pharmacology, 2024-08, Vol.90 (8), p.2004-2018

2024

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Discovery of Triazolopyrimidine Derivatives as Selective P2X3 Receptor Antagonists Binding to an Unprecedented Allosteric Site as Evidenced by Cryo-Electron Microscopy

Journal of medicinal chemistry, 2024-08, Vol.67 (16), p.14443-14465

2024

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Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists

Bioorganic & medicinal chemistry letters, 2021-11, Vol.52, p.128384-128384, Article 128384

2021

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BLU-5937: A selective P2X3 antagonist with potent anti-tussive effect and no taste alteration

Pulmonary pharmacology & therapeutics, 2019-06, Vol.56, p.56-62

2019

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Structural Basis of the Negative Allosteric Modulation of 5-BDBD at Human P2X4 Receptors

Molecular pharmacology, 2022-01, Vol.101 (1), p.33-44

2022

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P2X7-dependent, but differentially regulated release of IL-6, CCL2, and TNF-α in cultured mouse microglia

Glia, 2014-04, Vol.62 (4), p.592-607

2014

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Transient P2X7 Receptor Antagonism Produces Lasting Reductions in Spontaneous Seizures and Gliosis in Experimental Temporal Lobe Epilepsy

The Journal of neuroscience, 2016-06, Vol.36 (22), p.5920-5932

2016

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Neuroprotective and neuro-rehabilitative effects of acute purinergic receptor P2X4 (P2X4R) blockade after ischemic stroke

Experimental neurology, 2020-07, Vol.329, p.113308-113308, Article 113308

2020

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P2X7 receptor: an emerging target in central nervous system diseases

Trends in pharmacological sciences (Regular ed.), 2014-10, Vol.35 (10), p.537-547

2014

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4‑Methyl-6,7-dihydro‑4H‑triazolo[4,5‑c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate

Journal of medicinal chemistry, 2017-06, Vol.60 (11), p.4559-4572

2017

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Structure-Activity Relationships and Therapeutic Potential of Purinergic P2X7 Receptor Antagonists

Current medicinal chemistry, 2024-01, Vol.31 (11), p.1361-1403

2024

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Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP

Nature communications, 2016-02, Vol.7 (1), p.10555-10555, Article 10555

2016

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Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists

European journal of medicinal chemistry, 2021-12, Vol.226, p.113838-113838, Article 113838

2021

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Neuropsychopharmacology of JNJ-55308942: evaluation of a clinical candidate targeting P2X7 ion channels in animal models of neuroinflammation and anhedonia

Neuropsychopharmacology (New York, N.Y.), 2018-12, Vol.43 (13), p.2586-2596

2018

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Mapping the Site of Action of Human P2X7 Receptor Antagonists AZ11645373, Brilliant Blue G, KN-62, Calmidazolium, and ZINC58368839 to the Intersubunit Allosteric Pocket

Molecular pharmacology, 2019-09, Vol.96 (3), p.355-363

2019

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Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor

Neuroscience letters, 2019-01, Vol.690, p.219-224

2019

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Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ‐47965567

British journal of pharmacology, 2013-10, Vol.170 (3), p.624-640

2013

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Activation and regulation of purinergic P2X receptor channels

Action of MK‐7264 (gefapixant) at human P2X3 and P2X2/3 receptors and in vivo efficacy in models of sensitisation

Microglial P2X4R-evoked pain hypersensitivity is sexually dimorphic in rats

X-ray structures define human P2X(3) receptor gating cycle and antagonist action

Purinergic P2X receptors: Structural models and analysis of ligand-target interaction

The P2X7 receptor channel: recent developments and the use of P2X7 antagonists in models of disease

P2X7 receptor antagonism: Implications in diabetic retinopathy

P2X7 receptor in multifaceted cellular signalling and its relevance as a potential therapeutic target in different diseases

Pharmacodynamics, pharmacokinetics and CYP3A4 interaction potential of the selective P2X3 receptor antagonist filapixant: A randomized multiple ascending‐dose study in healthy young men

Discovery of Triazolopyrimidine Derivatives as Selective P2X3 Receptor Antagonists Binding to an Unprecedented Allosteric Site as Evidenced by Cryo-Electron Microscopy

Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists

BLU-5937: A selective P2X3 antagonist with potent anti-tussive effect and no taste alteration

Structural Basis of the Negative Allosteric Modulation of 5-BDBD at Human P2X4 Receptors

P2X7-dependent, but differentially regulated release of IL-6, CCL2, and TNF-α in cultured mouse microglia

Transient P2X7 Receptor Antagonism Produces Lasting Reductions in Spontaneous Seizures and Gliosis in Experimental Temporal Lobe Epilepsy

Neuroprotective and neuro-rehabilitative effects of acute purinergic receptor P2X4 (P2X4R) blockade after ischemic stroke

P2X7 receptor: an emerging target in central nervous system diseases

4‑Methyl-6,7-dihydro‑4H‑triazolo[4,5‑c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate

Structure-Activity Relationships and Therapeutic Potential of Purinergic P2X7 Receptor Antagonists

Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP

Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists

Neuropsychopharmacology of JNJ-55308942: evaluation of a clinical candidate targeting P2X7 ion channels in animal models of neuroinflammation and anhedonia

Mapping the Site of Action of Human P2X7 Receptor Antagonists AZ11645373, Brilliant Blue G, KN-62, Calmidazolium, and ZINC58368839 to the Intersubunit Allosteric Pocket

Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor

Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ‐47965567

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