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Critical Evaluation of P2X7 Receptor Antagonists in Selected Seizure Models

PloS one, 2016-06, Vol.11 (6), p.e0156468

2016

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Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432

The Journal of pharmacology and experimental therapeutics, 2014-12, Vol.351 (3), p.628

2014

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Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists

Bioorganic & medicinal chemistry letters, 2016-01, Vol.26 (2), p.257-261

2016

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Selective Inhibition of Orexin-2 Receptors Prevents Stress-Induced ACTH Release in Mice

Frontiers in behavioral neuroscience, 2017-05, Vol.11, p.83-83

2017

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The evolution of P2X7 antagonists with a focus on CNS indications

Bioorganic & medicinal chemistry letters, 2016-08, Vol.26 (16), p.3838-3845

2016

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JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats

Psychopharmacologia, 2011-04, Vol.214 (4), p.829-841

2011

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Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling

Bioorganic & medicinal chemistry, 2008-03, Vol.16 (6), p.2968-2973

2008

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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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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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A Dipolar Cycloaddition Reaction To Access 6‑Methyl-4,5,6,7-tetrahydro‑1H‑[1,2,3]triazolo[4,5‑c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate

Journal of medicinal chemistry, 2018-01, Vol.61 (1), p.207-223

2018

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Preclinical Evaluation of a P2X7 Receptor-Selective Radiotracer: PET Studies in a Rat Model with Local Overexpression of the Human P2X7 Receptor and in Nonhuman Primates

Journal of Nuclear Medicine, 2016-09, Vol.57 (9), p.1436-1441

2016

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Discovery of a Series of Substituted 1H‑((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators

Journal of medicinal chemistry, 2023-02, Vol.66 (4), p.2877-2892

2023

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Pharmacological characterization of JNJ-28583867, a histamine H3 receptor antagonist and serotonin reuptake inhibitor

European journal of pharmacology, 2007-12, Vol.576 (1-3), p.43-54

2007

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Discovery of a Series of Substituted 1 H -((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators

Journal of medicinal chemistry, 2023-02, Vol.66 (4), p.2877-2892

2023

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Design, Synthesis, and Preclinical Evaluation of 3‑Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5‑b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders

Journal of medicinal chemistry, 2020-09, Vol.63 (17), p.9181-9196

2020

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A novel radioligand for the ATP-gated ion channel P2X7: [3H] JNJ-54232334

European journal of pharmacology, 2015-10, Vol.765, p.551-559

2015

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Identification of (R)‑(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro‑1H‑imidazo[4,5‑c]pyridin-5(4H)‑yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor

Journal of medicinal chemistry, 2016-09, Vol.59 (18), p.8535-8548

2016

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Dual serotonin transporter/histamine H3 ligands : Optimization of the H3 pharmacophore

Bioorganic & medicinal chemistry letters, 2007-02, Vol.17 (3), p.702-706

2007

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Novel Octahydropyrrolo[3,4‑c]pyrroles Are Selective Orexin‑2 Antagonists: SAR Leading to a Clinical Candidate

Journal of medicinal chemistry, 2015-07, Vol.58 (14), p.5620-5636

2015

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Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists

Bioorganic & medicinal chemistry letters, 2015-08, Vol.25 (16), p.3157-3163

2015

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Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists

ACS medicinal chemistry letters, 2015-06, Vol.6 (6), p.671-676

2015

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Microwave assisted, palladium catalyzed aminocarbonylations of heteroaromatic bromides using solid Mo(CO) 6 as the carbon monoxide source

Tetrahedron letters, , Vol.48 (13), p.2339-2343

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1 H -Pyrrolo[3,2- b ]pyridine GluN2B-Selective Negative Allosteric Modulators

ACS medicinal chemistry letters, 2019-03, Vol.10 (3), p.261-266

2019

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Enantioselective Total Synthesis of Gracilins B and C Using Catalytic Asymmetric Diels-Alder Methodology

Journal of the American Chemical Society, 1995-09, Vol.117 (37), p.9616-9617

1995

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Critical Evaluation of P2X7 Receptor Antagonists in Selected Seizure Models

Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432

Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists

Selective Inhibition of Orexin-2 Receptors Prevents Stress-Induced ACTH Release in Mice

The evolution of P2X7 antagonists with a focus on CNS indications

JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats

Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling

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

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

A Dipolar Cycloaddition Reaction To Access 6‑Methyl-4,5,6,7-tetrahydro‑1H‑[1,2,3]triazolo[4,5‑c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate

Preclinical Evaluation of a P2X7 Receptor-Selective Radiotracer: PET Studies in a Rat Model with Local Overexpression of the Human P2X7 Receptor and in Nonhuman Primates

Discovery of a Series of Substituted 1H‑((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators

Pharmacological characterization of JNJ-28583867, a histamine H3 receptor antagonist and serotonin reuptake inhibitor

Discovery of a Series of Substituted 1 H -((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators

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

Design, Synthesis, and Preclinical Evaluation of 3‑Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5‑b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders

A novel radioligand for the ATP-gated ion channel P2X7: [3H] JNJ-54232334

Identification of (R)‑(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro‑1H‑imidazo[4,5‑c]pyridin-5(4H)‑yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor

Dual serotonin transporter/histamine H3 ligands : Optimization of the H3 pharmacophore

Novel Octahydropyrrolo[3,4‑c]pyrroles Are Selective Orexin‑2 Antagonists: SAR Leading to a Clinical Candidate

Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists

Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists

Microwave assisted, palladium catalyzed aminocarbonylations of heteroaromatic bromides using solid Mo(CO) 6 as the carbon monoxide source

1 H -Pyrrolo[3,2- b ]pyridine GluN2B-Selective Negative Allosteric Modulators

Enantioselective Total Synthesis of Gracilins B and C Using Catalytic Asymmetric Diels-Alder Methodology

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