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Literature DB >> 23421671

Is there a path forward for mGlu(2) positive allosteric modulators for the treatment of schizophrenia?

Abstract

Two recent Phase II results show opposing outcomes for the potential of activators of mGlu2 in the treatment of schizophrenia. The first outcome revealed that Eli Lilly's mGlu2/3 agonist, pomaglumetad methionil (LY2140023), failed to meet the primary efficacy end point. The second report showed the mGlu2 positive allosteric modulator (PAM) from Addex (ADX71149) in conjunction with Janssen Research & Development met the primary objectives of safety, tolerability and demonstrated an effect on negative symptoms in patients.

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Year: 2013 PMID： 23421671 PMCID： PMC3582287 DOI： 10.1021/cn400023y

Source DB: PubMed Journal: ACS Chem Neurosci ISSN： 1948-7193 Impact factor: 4.418

11 in total

1. Imidazo[1,2-a]pyridines: orally active positive allosteric modulators of the metabotropic glutamate 2 receptor.

Authors: Andrés A Trabanco; Gary Tresadern; Gregor J Macdonald; Juan Antonio Vega; Ana Isabel de Lucas; Encarnación Matesanz; Aránzazu García; María Lourdes Linares; Sergio A Alonso de Diego; José Manuel Alonso; Daniel Oehlrich; Abdelah Ahnaou; Wilhelmus Drinkenburg; Claire Mackie; José Ignacio Andrés; Hilde Lavreysen; José María Cid
Journal: J Med Chem Date: 2012-03-01 Impact factor: 7.446

2. Discovery of 1,5-disubstituted pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor.

Authors: Jose María Cid; Guillaume Duvey; Philippe Cluzeau; Vanthea Nhem; Karim Macary; Alexandre Raux; Nicolas Poirier; Jessica Muller; Christelle Boléa; Terry Finn; Sonia Poli; Mark Epping-Jordan; Emilie Chamelot; Francis Derouet; Francoise Girard; Gregor J Macdonald; Juan Antonio Vega; Ana Isabel de Lucas; Encarnación Matesanz; Hilde Lavreysen; María Lourdes Linares; Daniel Oehlrich; Julen Oyarzábal; Gary Tresadern; Andrés A Trabanco; Jose Ignacio Andrés; Emmanuel Le Poul; Hassan Imogai; Robert Lutjens; Jean-Philippe Rocher
Journal: ACS Chem Neurosci Date: 2010-08-23 Impact factor: 4.418

Review 3. From revolution to evolution: the glutamate hypothesis of schizophrenia and its implication for treatment.

Authors: Bita Moghaddam; Daniel Javitt
Journal: Neuropsychopharmacology Date: 2011-09-28 Impact factor: 7.853

4. New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): identification and synthesis of N-propyl-8-chloro-6-substituted isoquinolones.

Authors: Andrés A Trabanco; Guillaume Duvey; José María Cid; Gregor J Macdonald; Philippe Cluzeau; Vanthea Nhem; Rocco Furnari; Nadia Behaj; Géraldine Poulain; Terry Finn; Hilde Lavreysen; Sonia Poli; Alexandre Raux; Yves Thollon; Nicolas Poirier; David D'Addona; José Ignacio Andrés; Robert Lutjens; Emmanuel Le Poul; Hassan Imogai; Jean-Philippe Rocher
Journal: Bioorg Med Chem Lett Date: 2010-12-21 Impact factor: 2.823

5. Synthesis, evaluation, and radiolabeling of new potent positive allosteric modulators of the metabotropic glutamate receptor 2 as potential tracers for positron emission tomography imaging.

Authors: José-Ignacio Andrés; Jesús Alcázar; José María Cid; Meri De Angelis; Laura Iturrino; Xavier Langlois; Hilde Lavreysen; Andrés A Trabanco; Sofie Celen; Guy Bormans
Journal: J Med Chem Date: 2012-10-11 Impact factor: 7.446

6. The economic burden of schizophrenia in the United States in 2002.

Authors: Eric Q Wu; Howard G Birnbaum; Lizheng Shi; Daniel E Ball; Ronald C Kessler; Matthew Moulis; Jyoti Aggarwal
Journal: J Clin Psychiatry Date: 2005-09 Impact factor: 4.384

7. Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: a randomized Phase 2 clinical trial.

Authors: Sandeep T Patil; Lu Zhang; Ferenc Martenyi; Stephen L Lowe; Kimberley A Jackson; Boris V Andreev; Alla S Avedisova; Leonid M Bardenstein; Issak Y Gurovich; Margarita A Morozova; Sergey N Mosolov; Nikolai G Neznanov; Alexander M Reznik; Anatoly B Smulevich; Vladimir A Tochilov; Bryan G Johnson; James A Monn; Darryle D Schoepp
Journal: Nat Med Date: 2007-09-02 Impact factor: 53.440

8. Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): a positive allosteric modulator of the metabotropic glutamate 2 receptor.

Authors: Jose María Cid; Gary Tresadern; Juan Antonio Vega; Ana Isabel de Lucas; Encarnación Matesanz; Laura Iturrino; María Lourdes Linares; Aránzazu Garcia; José Ignacio Andrés; Gregor J Macdonald; Daniel Oehlrich; Hilde Lavreysen; Anton Megens; Abdellah Ahnaou; Wilhelmus Drinkenburg; Claire Mackie; Stefan Pype; David Gallacher; Andrés A Trabanco
Journal: J Med Chem Date: 2012-10-16 Impact factor: 7.446

9. Scaffold hopping from pyridones to imidazo[1,2-a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor.

Authors: Gary Tresadern; Jose María Cid; Gregor J Macdonald; Juan Antonio Vega; Ana Isabel de Lucas; Aránzazu García; Encarnación Matesanz; María Lourdes Linares; Daniel Oehlrich; Hilde Lavreysen; Ilse Biesmans; Andrés A Trabanco
Journal: Bioorg Med Chem Lett Date: 2009-11-10 Impact factor: 2.823

10. Corticolimbic dopamine neurotransmission is temporally dissociated from the cognitive and locomotor effects of phencyclidine.

Authors: B Adams; B Moghaddam
Journal: J Neurosci Date: 1998-07-15 Impact factor: 6.167

17 in total

Review 1. Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.

Authors: Craig W Lindsley; Kyle A Emmitte; Corey R Hopkins; Thomas M Bridges; Karen J Gregory; Colleen M Niswender; P Jeffrey Conn
Journal: Chem Rev Date: 2016-02-16 Impact factor: 60.622

Review 2. Perspectives on the mGluR2/3 agonists as a therapeutic target for schizophrenia: Still promising or a dead end?

Authors: Meng-Lin Li; Xi-Quan Hu; Feng Li; Wen-Jun Gao
Journal: Prog Neuropsychopharmacol Biol Psychiatry Date: 2015-02-24 Impact factor: 5.067

Review 3. Computational Advances for the Development of Allosteric Modulators and Bitopic Ligands in G Protein-Coupled Receptors.

Authors: Zhiwei Feng; Guanxing Hu; Shifan Ma; Xiang-Qun Xie
Journal: AAPS J Date: 2015-05-05 Impact factor: 4.009

4. Allosteric Binding Site and Activation Mechanism of Class C G-Protein Coupled Receptors: Metabotropic Glutamate Receptor Family.

Authors: Zhiwei Feng; Shifan Ma; Guanxing Hu; Xiang-Qun Xie
Journal: AAPS J Date: 2015-03-12 Impact factor: 4.009

Review 5. Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders.

Authors: Daniel J Foster; P Jeffrey Conn
Journal: Neuron Date: 2017-05-03 Impact factor: 17.173

Review 10. The Role of G Protein-Coupled Receptors (GPCRs) and Calcium Signaling in Schizophrenia. Focus on GPCRs Activated by Neurotransmitters and Chemokines.

Authors: Tomasz Boczek; Joanna Mackiewicz; Marta Sobolczyk; Julia Wawrzyniak; Malwina Lisek; Bozena Ferenc; Feng Guo; Ludmila Zylinska
Journal: Cells Date: 2021-05-17 Impact factor: 6.600