Publications by authors named "Michael Letavic"

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Characterization of tritiated JNJ-GluN2B-5 (3-[H] 1-(azetidin-1-yl)-2-(6-(4-fluoro-3-methyl-phenyl)pyrrolo[3,2-b]pyridin-1-yl)ethanone), a high affinity GluN2B radioligand with selectivity over sigma receptors.
Jeffrey Schoellerman, Brian Lord, Anindya Bhattacharya, Brice Stenne, Jessica L Wall, Michael Letavic

J Neurochem· September 2024

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Molecular determinants of ASIC1 modulation by divalent cations.
Yi Liu, Jichun Ma, Renee L DesJarlais, Rebecca Hagan, Jason Rech, Michael Letavic

Sci Rep· January 2024

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Discovery of a Series of Substituted 1-((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators.
Christine F Gelin, Brice Stenne, Heather Coate, Afton Hiscox, Akinola Soyode-Johnson, Michael A Letavic

J Med Chem· February 2023

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Molecular mechanism and structural basis of small-molecule modulation of the gating of acid-sensing ion channel 1.
Yi Liu, Jichun Ma, Renee L DesJarlais, Rebecca Hagan, Jason Rech, Michael Letavic

Commun Biol· February 2021

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P2X7 receptor antagonists for the treatment of systemic inflammatory disorders.
Christine F Gelin, Anindya Bhattacharya, Michael A Letavic

Prog Med Chem· November 2020

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Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders.
Christa C Chrovian, Akinola Soyode-Johnson, Brice Stenne, Daniel J Pippel, Jeffrey Schoellerman, Michael A Letavic

J Med Chem· September 2020

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PET Imaging of the P2X7 Ion Channel with a Novel Tracer [F]JNJ-64413739 in a Rat Model of Neuroinflammation.
Tamara Berdyyeva, Chunfang Xia, Natalie Taylor, Yingbo He, Gang Chen, Michael Letavic

Mol Imaging Biol· October 2019

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Preclinical Evaluation and Nonhuman Primate Receptor Occupancy Study of F-JNJ-64413739, a PET Radioligand for P2X7 Receptors.
Hartmuth C Kolb, Olivier Barret, Anindya Bhattacharya, Gang Chen, Cristian Constantinescu, Michael Letavic

J Nucl Med· August 2019

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1-Pyrrolo[3,2-]pyridine GluN2B-Selective Negative Allosteric Modulators.
Christa C Chrovian, Akinola Soyode-Johnson, Jessica L Wall, Jason C Rech, Jeff Schoellerman, Michael A Letavic

ACS Med Chem Lett· March 2019

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Neuropsychopharmacology of JNJ-55308942: evaluation of a clinical candidate targeting P2X7 ion channels in animal models of neuroinflammation and anhedonia.
Anindya Bhattacharya, Brian Lord, Jan-Sebastian Grigoleit, Yingbo He, Ian Fraser, Michael A Letavic

Neuropsychopharmacology· December 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.
Christa C Chrovian, Akinola Soyode-Johnson, Alexander A Peterson, Christine F Gelin, Xiaohu Deng, Michael A Letavic

J Med Chem· January 2018

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Critical Evaluation of P2X7 Receptor Antagonists in Selected Seizure Models.
Wolfgang Fischer, Heike Franke, Ute Krügel, Heiko Müller, Klaus Dinkel, Michael A Letavic

PLoS One· July 2017

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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.
Michael A Letavic, Brad M Savall, Brett D Allison, Leah Aluisio, Jose Ignacio Andres

J Med Chem· June 2017

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Selective Inhibition of Orexin-2 Receptors Prevents Stress-Induced ACTH Release in Mice.
Sujin Yun, Michelle Wennerholm, Jonathan E Shelton, Pascal Bonaventure, Michael A Letavic

Front Behav Neurosci· May 2017

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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.
Dieter Ory, Sofie Celen, Rik Gijsbers, Chris Van Den Haute, Andrey Postnov, Michael A Letavic

J Nucl Med· September 2016

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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.
Devin M Swanson, Brad M Savall, Kevin J Coe, Freddy Schoetens, Tatiana Koudriakova, Michael A Letavic

J Med Chem· September 2016

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The evolution of P2X7 antagonists with a focus on CNS indications.
Jason C Rech, Anindya Bhattacharya, Michael A Letavic, Brad M Savall

Bioorg Med Chem Lett· August 2016

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Transient P2X7 Receptor Antagonism Produces Lasting Reductions in Spontaneous Seizures and Gliosis in Experimental Temporal Lobe Epilepsy.
Alba Jimenez-Pacheco, Miguel Diaz-Hernandez, Marina Arribas-Blázquez, Amaya Sanz-Rodriguez, Luis A Olivos-Oré, Michael Letavic

J Neurosci· June 2016

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Novel Phenyl-Substituted 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 Antagonists with Robust Target Engagement in Rat Brain.
Christa C Chrovian, Akinola Soyode-Johnson, Hong Ao, Genesis M Bacani, Nicholas I Carruthers, Michael A Letavic

ACS Chem Neurosci· April 2016

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Substituted 5,6-(Dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-methanones as P2X7 Antagonists.
Jeannie Ziff, Dale A Rudolph, Brice Stenne, Tatiana Koudriakova, Brian Lord, Michael A Letavic

ACS Chem Neurosci· April 2016

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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.
Michael K Ameriks, Hong Ao, Nicholas I Carruthers, Brian Lord, Suchitra Ravula, Michael A Letavic

Bioorg Med Chem Lett· January 2016

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microRNA targeting of the P2X7 purinoceptor opposes a contralateral epileptogenic focus in the hippocampus.
Eva M Jimenez-Mateos, Marina Arribas-Blazquez, Amaya Sanz-Rodriguez, Caoimhin Concannon, Luis A Olivos-Ore, Michael Letavic

Sci Rep· December 2015

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A novel radioligand for the ATP-gated ion channel P2X7: [3H] JNJ-54232334.
Brian Lord, Michael K Ameriks, Qi Wang, Lawrence Fourgeaud, Maarten Vliegen, Michael A Letavic

Eur J Pharmacol· October 2015

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Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia.
Pascal Bonaventure, Jonathan Shelton, Sujin Yun, Diane Nepomuceno, Steven Sutton, Michael Letavic

J Pharmacol Exp Ther· September 2015

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Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists.
Brad M Savall, Duncan Wu, Meri De Angelis, Nicholas I Carruthers, Hong Ao, Michael A Letavic

ACS Med Chem Lett· June 2015

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