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mGlu5 negative allosteric modulators: a patent review (2010 – 2012)

Pages 393-408 | Published online: 22 Jan 2013

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Kyle A. Emmitte. (2017) mGlu5 negative allosteric modulators: a patent review (2013 - 2016). Expert Opinion on Therapeutic Patents 27:6, pages 691-706.
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Dmitry Petrov, Ignacio Pedros, Maria Luisa de Lemos, Mercè Pallàs, Anna Maria Canudas, Alberto Lazarowski, Carlos Beas-Zarate, Carme Auladell, Jaume Folch & Antoni Camins. (2014) Mavoglurant as a treatment for Parkinson’s disease. Expert Opinion on Investigational Drugs 23:8, pages 1165-1179.
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Ting-ting Fu, Gao Tu, Meng Ping, Guo-xun Zheng, Feng-yuan Yang, Jing-yi Yang, Yang Zhang, Xiao-jun Yao, Wei-wei Xue & Feng Zhu. (2020) Subtype-selective mechanisms of negative allosteric modulators binding to group I metabotropic glutamate receptors. Acta Pharmacologica Sinica 42:8, pages 1354-1367.
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Kirstie A. Bennett, Eugenia Sergeev, Cliona P. MacSweeney, Geor Bakker & Anne E. Cooper. (2021) Understanding Exposure-Receptor Occupancy Relationships for Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators across a Range of Preclinical and Clinical Studies. Journal of Pharmacology and Experimental Therapeutics 377:1, pages 157-168.
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Shaoyong Lu & Jian Zhang. (2018) Small Molecule Allosteric Modulators of G-Protein-Coupled Receptors: Drug–Target Interactions. Journal of Medicinal Chemistry 62:1, pages 24-45.
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Phuc N.H. Trinh, Lauren T. May, Katie Leach & Karen J. Gregory. (2018) Biased agonism and allosteric modulation of metabotropic glutamate receptor 5. Clinical Science 132:21, pages 2323-2338.
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Tingting Fu, Guoxun Zheng, Gao Tu, Fengyuan Yang, Yuzong Chen, Xiaojun Yao, Xiaofeng Li, Weiwei Xue & Feng Zhu. (2018) Exploring the Binding Mechanism of Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators in Clinical Trials by Molecular Dynamics Simulations. ACS Chemical Neuroscience 9:6, pages 1492-1502.
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Samuel A. Barnes, Douglas J. Sheffler, Svetlana Semenova, Nicholas D.P. Cosford & Anton Bespalov. (2018) Metabotropic Glutamate Receptor 5 as a Target for the Treatment of Depression and Smoking: Robust Preclinical Data but Inconclusive Clinical Efficacy. Biological Psychiatry 83:11, pages 955-962.
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Khaled S. Abd-Elrahman, Alison Hamilton, Shaunessy R. Hutchinson, Fang LiuRyan C. RussellStephen S. G. Ferguson. (2017) mGluR5 antagonism increases autophagy and prevents disease progression in the zQ175 mouse model of Huntington’s disease . Science Signaling 10:510.
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Wataru Hirose, Yoshihiro Kato, Itaru Natsutani, Makoto Takata, Maiko Kitaichi, Satoki Imai, Shun Hayashi, Yukiyo Arai, Kohei Hoshino & Kohzo Yoshida. (2017) Synthesis and optimization of 4,5,6,7-tetrahydrooxazolo[4,5-c]pyridines as potent and orally-active metabotropic glutamate receptor 5 negative allosteric modulators. Bioorganic & Medicinal Chemistry Letters 27:18, pages 4331-4335.
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Valerio D'Amore, Renée H.L. Raaijmakers, Ines Santolini, Clementina M. van Rijn, Richard Teke Ngomba, Ferdinando Nicoletti & Gilles van Luijtelaar. (2016) The anti-absence effect of mGlu5 receptor amplification with VU0360172 is maintained during and after antiepileptogenesis. Pharmacology Biochemistry and Behavior 146-147, pages 50-59.
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Rajapillai L. I. Pillai & Dnyanesh N. Tipre. (2016) Metabotropic glutamate receptor 5 ? a promising target in drug development and neuroimaging. European Journal of Nuclear Medicine and Molecular Imaging 43:6, pages 1151-1170.
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Gopinath S. Palanisamy, John M. Marcek, Gregg D. Cappon, Jessica Whritenour, Christopher L. Shaffer, Joseph T. Brady & Christopher Houle. (2015) Drug-induced Skin Lesions in Cynomolgus Macaques Treated with Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulators. Toxicologic Pathology 43:7, pages 995-1003.
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Kasper Harpsøe, Vignir Isberg, Benjamin G. Tehan, Dahlia Weiss, Angela Arsova, Fiona H. Marshall, Hans Bräuner-Osborne & David E. Gloriam. (2015) Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants. Scientific Reports 5:1.
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Zhiwei Feng, Shifan Ma, Guanxing Hu & Xiang-Qun Xie. (2015) Allosteric Binding Site and Activation Mechanism of Class C G-Protein Coupled Receptors: Metabotropic Glutamate Receptor Family. The AAPS Journal 17:3, pages 737-753.
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Lei Zhang, Gayatri Balan, Gabriela Barreiro, Brian P. Boscoe, Lois K. Chenard, Julie Cianfrogna, Michelle M. Claffey, Laigao Chen, Karen J. Coffman, Susan E. Drozda, Joshua R. Dunetz, Kari R. Fonseca, Paul Galatsis, Sarah Grimwood, John T. Lazzaro, Jessica Y. Mancuso, Emily L. Miller, Matthew R. Reese, Bruce N. Rogers, Isao Sakurada, Marc Skaddan, Deborah L. Smith, Antonia F. Stepan, Patrick Trapa, Jamison B. Tuttle, Patrick R. Verhoest, Daniel P. Walker, Ann S. Wright, Margaret M. Zaleska, Kenneth Zasadny & Christopher L. Shaffer. (2014) Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1 H -pyrazolo-[3,4- b ]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator . Journal of Medicinal Chemistry 57:3, pages 861-877.
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Andrew S. Felts, Alice L. Rodriguez, Ryan D. Morrison, Daryl F. Venable, Jason T. Manka, Brittney S. Bates, Anna L. Blobaum, Frank W. Byers, J. Scott Daniels, Colleen M. Niswender, Carrie K. Jones, P. Jeffrey Conn, Craig W. Lindsley & Kyle A. Emmitte. (2013) Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorganic & Medicinal Chemistry Letters 23:21, pages 5779-5785.
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Russell J. Amato, Andrew S. Felts, Alice L. Rodriguez, Daryl F. Venable, Ryan D. Morrison, Frank W. Byers, J. Scott Daniels, Colleen M. Niswender, P. Jeffrey Conn, Craig W. Lindsley, Carrie K. Jones & Kyle A. Emmitte. (2013) Substituted 1-Phenyl-3-(pyridin-2-yl)urea Negative Allosteric Modulators of mGlu 5 : Discovery of a New Tool Compound VU0463841 with Activity in Rat Models of Cocaine Addiction . ACS Chemical Neuroscience 4:8, pages 1217-1228.
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