Critical Evaluation of P2X7 Receptor Antagonists in Selected Seizure Models
Fischer, Wolfgang, Franke, Heike, Krügel, Ute, Müller, Heiko, Dinkel, Klaus, Lord, Brian, Letavic, Michael A, Henshall, David C, Engel, Tobias
Published in PloS one (09.06.2016)
Published in PloS one (09.06.2016)
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Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432
Lord, Brian, Aluisio, Leah, Shoblock, James R, Neff, Robert A, Varlinskaya, Elena I, Ceusters, Marc, Lovenberg, Timothy W, Carruthers, Nicholas, Bonaventure, Pascal, Letavic, Michael A, Deak, Terrence, Drinkenburg, Wilhelmus, Bhattacharya, Anindya
Published in The Journal of pharmacology and experimental therapeutics (01.12.2014)
Published in The Journal of pharmacology and experimental therapeutics (01.12.2014)
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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
Ameriks, Michael K., Ao, Hong, Carruthers, Nicholas I., Lord, Brian, Ravula, Suchitra, Rech, Jason C., Savall, Brad M., Wall, Jessica L., Wang, Qi, Bhattacharya, Anindya, Letavic, Michael A.
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
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Selective Inhibition of Orexin-2 Receptors Prevents Stress-Induced ACTH Release in Mice
Yun, Sujin, Wennerholm, Michelle, Shelton, Jonathan E, Bonaventure, Pascal, Letavic, Michael A, Shireman, Brock T, Lovenberg, Timothy W, Dugovic, Christine
Published in Frontiers in behavioral neuroscience (08.05.2017)
Published in Frontiers in behavioral neuroscience (08.05.2017)
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JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats
Galici, Ruggero, Rezvani, Amir H., Aluisio, Leah, Lord, Brian, Levin, Edward D., Fraser, Ian, Boggs, Jamin, Welty, Natalie, Shoblock, James R., Motley, S. Timothy, Letavic, Michael A., Carruthers, Nicholas I., Dugovic, Christine, Lovenberg, Timothy W., Bonaventure, Pascal
Published in Psychopharmacologia (01.04.2011)
Published in Psychopharmacologia (01.04.2011)
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Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling
BEMBENEK, Scott D, KEITH, John M, LETAVIC, Michael A, APODACA, Richard, BARBIER, Ann J, DVORAK, Lisa, ALUISIO, Leah, MILLER, Kirsten L, LOVENBERG, Timothy W, CARRUTHERS, Nicholas I
Published in Bioorganic & medicinal chemistry (15.03.2008)
Published in Bioorganic & medicinal chemistry (15.03.2008)
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The evolution of P2X7 antagonists with a focus on CNS indications
Rech, Jason C., Bhattacharya, Anindya, Letavic, Michael A., Savall, Brad M.
Published in Bioorganic & medicinal chemistry letters (15.08.2016)
Published in Bioorganic & medicinal chemistry letters (15.08.2016)
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Pharmacological characterization of JNJ-28583867, a histamine H3 receptor antagonist and serotonin reuptake inhibitor
BARBIER, Ann J, ALUISIO, Leah, PUDIAK, Cindy, DUGOVIC, Christine, SHELTON, Jonathan, MAZUR, Curt, LETAVIC, Michael A, CARRUTHERS, Nicholas I, LOVENBERG, Timothy W, LORD, Brian, YING QU, WILSON, Sandy J, BOGGS, Jamin D, BONAVENTURE, Pascal, MILLER, Kirsten, FRASER, Ian, DVORAK, Lisa
Published in European journal of pharmacology (01.12.2007)
Published in European journal of pharmacology (01.12.2007)
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Neuropsychopharmacology of JNJ-55308942: evaluation of a clinical candidate targeting P2X7 ion channels in animal models of neuroinflammation and anhedonia
Bhattacharya, Anindya, Lord, Brian, Grigoleit, Jan-Sebastian, He, Yingbo, Fraser, Ian, Campbell, Shannon N, Taylor, Natalie, Aluisio, Leah, O'Connor, Jason C, Papp, Mariusz, Chrovian, Christa, Carruthers, Nicholas, Lovenberg, Timothy W, Letavic, Michael A
Published in Neuropsychopharmacology (New York, N.Y.) (01.12.2018)
Published in Neuropsychopharmacology (New York, N.Y.) (01.12.2018)
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Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ‐47965567
Bhattacharya, Anindya, Wang, Qi, Ao, Hong, Shoblock, James R, Lord, Brian, Aluisio, Leah, Fraser, Ian, Nepomuceno, Diane, Neff, Robert A, Welty, Natalie, Lovenberg, Timothy W, Bonaventure, Pascal, Wickenden, Alan D, Letavic, Michael A
Published in British journal of pharmacology (01.10.2013)
Published in British journal of pharmacology (01.10.2013)
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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
Chrovian, Christa C, Soyode-Johnson, Akinola, Peterson, Alexander A, Gelin, Christine F, Deng, Xiaohu, Dvorak, Curt A, Carruthers, Nicholas I, Lord, Brian, Fraser, Ian, Aluisio, Leah, Coe, Kevin J, Scott, Brian, Koudriakova, Tatiana, Schoetens, Freddy, Sepassi, Kia, Gallacher, David J, Bhattacharya, Anindya, Letavic, Michael A
Published in Journal of medicinal chemistry (11.01.2018)
Published in Journal of medicinal chemistry (11.01.2018)
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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
Ory, Dieter, Celen, Sofie, Gijsbers, Rik, Van Den Haute, Chris, Postnov, Andrey, Koole, Michel, Vandeputte, Caroline, Andrés, José-Ignacio, Alcazar, Jesus, De Angelis, Meri, Langlois, Xavier, Bhattacharya, Anindya, Schmidt, Mark, Letavic, Michael A, Vanduffel, Wim, Van Laere, Koen, Verbruggen, Alfons, Debyser, Zeger, Bormans, Guy
Published in Journal of Nuclear Medicine (01.09.2016)
Published in Journal of Nuclear Medicine (01.09.2016)
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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
Gelin, Christine F., Stenne, Brice, Coate, Heather, Hiscox, Afton, Soyode-Johnson, Akinola, Wall, Jessica L., Lord, Brian, Schoellerman, Jeffrey, Coe, Kevin J., Wang, Kai, Alcázar, Jesus, Chrovian, Christa C., Dvorak, Curt A., Carruthers, Nicholas I., Koudriakova, Tatiana, Balana, Bartosz, Letavic, Michael A.
Published in Journal of medicinal chemistry (23.02.2023)
Published in Journal of medicinal chemistry (23.02.2023)
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Dual serotonin transporter/histamine H3 ligands : Optimization of the H3 pharmacophore
KEITH, John M, GOMEZ, Leslie A, MAZUR, Curt, LOVENBERG, Timothy W, CARRUTHERS, Nicholas I, LETAVIC, Michael A, LY, Kiev S, JABLONOWSKI, Jill A, SEIERSTAD, Mark, BARBIER, Ann J, WILSON, Sandy J, BOGGS, Jamin D, FRASER, Ian C
Published in Bioorganic & medicinal chemistry letters (01.02.2007)
Published in Bioorganic & medicinal chemistry letters (01.02.2007)
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Journal Article
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
Gelin, Christine F, Stenne, Brice, Coate, Heather, Hiscox, Afton, Soyode-Johnson, Akinola, Wall, Jessica L, Lord, Brian, Schoellerman, Jeffrey, Coe, Kevin J, Wang, Kai, Alcázar, Jesus, Chrovian, Christa C, Dvorak, Curt A, Carruthers, Nicholas I, Koudriakova, Tatiana, Balana, Bartosz, Letavic, Michael A
Published in Journal of medicinal chemistry (23.02.2023)
Published in Journal of medicinal chemistry (23.02.2023)
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Journal Article
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
Letavic, Michael A, Savall, Brad M, Allison, Brett D, Aluisio, Leah, Andres, Jose Ignacio, De Angelis, Meri, Ao, Hong, Beauchamp, Derek A, Bonaventure, Pascal, Bryant, Stewart, Carruthers, Nicholas I, Ceusters, Marc, Coe, Kevin J, Dvorak, Curt A, Fraser, Ian C, Gelin, Christine F, Koudriakova, Tatiana, Liang, Jimmy, Lord, Brian, Lovenberg, Timothy W, Otieno, Monicah A, Schoetens, Freddy, Swanson, Devin M, Wang, Qi, Wickenden, Alan D, Bhattacharya, Anindya
Published in Journal of medicinal chemistry (08.06.2017)
Published in Journal of medicinal chemistry (08.06.2017)
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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
Chrovian, Christa C, Soyode-Johnson, Akinola, Stenne, Brice, Pippel, Daniel J, Schoellerman, Jeffrey, Lord, Brian, Needham, Alexandra S, Xia, Chungfang, Coe, Kevin J, Sepassi, Kia, Schoetens, Freddy, Scott, Brian, Nguyen, Leslie, Jiang, Xiaohui, Koudriakova, Tatiana, Balana, Bartosz, Letavic, Michael A
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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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
Swanson, Devin M, Savall, Brad M, Coe, Kevin J, Schoetens, Freddy, Koudriakova, Tatiana, Skaptason, Judith, Wall, Jessica, Rech, Jason, Deng, Xiahou, De Angelis, Meri, Everson, Anita, Lord, Brian, Wang, Qi, Ao, Hong, Scott, Brian, Sepassi, Kia, Lovenberg, Timothy W, Carruthers, Nicholas I, Bhattacharya, Anindya, Letavic, Michael A
Published in Journal of medicinal chemistry (22.09.2016)
Published in Journal of medicinal chemistry (22.09.2016)
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A novel radioligand for the ATP-gated ion channel P2X7: [3H] JNJ-54232334
Lord, Brian, Ameriks, Michael K., Wang, Qi, Fourgeaud, Lawrence, Vliegen, Maarten, Verluyten, Willy, Haspeslagh, Pieter, Carruthers, Nicholas I., Lovenberg, Timothy W., Bonaventure, Pascal, Letavic, Michael A., Bhattacharya, Anindya
Published in European journal of pharmacology (15.10.2015)
Published in European journal of pharmacology (15.10.2015)
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