Literature DB >> 29259756

VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides.

Carson W Reed1, Kevin M McGowan1, Paul K Spearing1, Branden J Stansley1, Hanna F Roenfanz1, Darren W Engers1, Alice L Rodriguez1, Eileen M Engelberg1, Vincent B Luscombe1, Matthew T Loch1, Daniel H Remke1, Jerri M Rook1, Anna L Blobaum1, P Jeffrey Conn1,2, Colleen M Niswender1,2, Craig W Lindsley1,1.   

Abstract

Herein, we report the structure-activity relationships within a series of mGlu7 NAMs based on an N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamide core with excellent CNS penetration (Kp 1.9-5.8 and Kp,uu 0.4-1.4). Analogues in this series displayed steep SAR. Of these, VU6010608 (11a) emerged with robust efficacy in blocking high frequency stimulated long-term potentiation in electrophysiology studies.

Entities:  

Year:  2017        PMID： 29259756      PMCID： PMC5733308          DOI： 10.1021/acsmedchemlett.7b00429

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  22 in total

1.  Lack of the metabotropic glutamate receptor subtype 7 selectively modulates Theta rhythm and working memory.

Authors:  Christian Hölscher; Susanne Schmid; Peter K D Pilz; Gilles Sansig; Herman van der Putten; Claudia F Plappert
Journal:  Learn Mem       Date:  2005 Sep-Oct       Impact factor: 2.460

2.  mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome.

Authors:  Rocco G Gogliotti; Rebecca K Senter; Nicole M Fisher; Jeffrey Adams; Rocio Zamorano; Adam G Walker; Anna L Blobaum; Darren W Engers; Corey R Hopkins; J Scott Daniels; Carrie K Jones; Craig W Lindsley; Zixiu Xiang; P Jeffrey Conn; Colleen M Niswender
Journal:  Sci Transl Med       Date:  2017-08-16       Impact factor: 17.956

3.  Concomitant deficits in working memory and fear extinction are functionally dissociated from reduced anxiety in metabotropic glutamate receptor 7-deficient mice.

Authors:  Zsuzsanna Callaerts-Vegh; Tom Beckers; Simon M Ball; Frank Baeyens; Patrick F Callaerts; John F Cryan; Elek Molnar; Rudi D'Hooge
Journal:  J Neurosci       Date:  2006-06-14       Impact factor: 6.167

4.  Increased seizure susceptibility in mice lacking metabotropic glutamate receptor 7.

Authors:  G Sansig; T J Bushell; V R Clarke; A Rozov; N Burnashev; C Portet; F Gasparini; M Schmutz; K Klebs; R Shigemoto; P J Flor; R Kuhn; T Knoepfel; M Schroeder; D R Hampson; V J Collett; C Zhang; R M Duvoisin; G L Collingridge; H van Der Putten
Journal:  J Neurosci       Date:  2001-11-15       Impact factor: 6.167

5.  Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7.

Authors:  Colleen M Niswender; Kari A Johnson; Nicole R Miller; Jennifer E Ayala; Qingwei Luo; Richard Williams; Samir Saleh; Darren Orton; C David Weaver; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2009-12-21       Impact factor: 4.436

Review 6.  Metabotropic glutamate receptors: physiology, pharmacology, and disease.

Authors:  Colleen M Niswender; P Jeffrey Conn
Journal:  Annu Rev Pharmacol Toxicol       Date:  2010       Impact factor: 13.820

7.  Deficits in acquisition and extinction of conditioned responses in mGluR7 knockout mice.

Authors:  Hannelore Goddyn; Zsuzsanna Callaerts-Vegh; Stijn Stroobants; Trinette Dirikx; Debora Vansteenwegen; Dirk Hermans; Herman van der Putten; Rudi D'Hooge
Journal:  Neurobiol Learn Mem       Date:  2008-03-04       Impact factor: 2.877

8.  Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines.

Authors:  Masahito Abe; Mabel Seto; Rocco G Gogliotti; Matthew T Loch; Katrina A Bollinger; Sichen Chang; Eileen M Engelberg; Vincent B Luscombe; Joel M Harp; Michael Bubser; Darren W Engers; Carrie K Jones; Alice L Rodriguez; Anna L Blobaum; P Jeffrey Conn; Colleen M Niswender; Craig W Lindsley
Journal:  ACS Med Chem Lett       Date:  2017-09-01       Impact factor: 4.345

9.  Altered short-term synaptic plasticity in mice lacking the metabotropic glutamate receptor mGlu7.

Authors:  Trevor J Bushell; Gilles Sansig; Valerie J Collett; Herman van der Putten; Graham L Collingridge
Journal:  ScientificWorldJournal       Date:  2002-03-15

10.  Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7.

Authors:  Nidhi Jalan-Sakrikar; Julie R Field; Rebecca Klar; Margrith E Mattmann; Karen J Gregory; Rocio Zamorano; Darren W Engers; Sean R Bollinger; C David Weaver; Emily L Days; L Michelle Lewis; Thomas J Utley; Miguel Hurtado; Delphine Rigault; Francine Acher; Adam G Walker; Bruce J Melancon; Michael R Wood; Craig W Lindsley; P Jeffrey Conn; Zixiu Xiang; Corey R Hopkins; Colleen M Niswender
Journal:  ACS Chem Neurosci       Date:  2014-10-09       Impact factor: 4.418
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  7 in total

1.  Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu7 Positive Allosteric Modulator Tool Compound.

Authors:  Carson W Reed; Jacob J Kalbfleisch; Madison J Wong; Jordan P Washecheck; Ashton Hunter; Alice L Rodriguez; Anna L Blobaum; P Jeffrey Conn; Colleen M Niswender; Craig W Lindsley
Journal:  ACS Med Chem Lett       Date:  2020-08-20       Impact factor: 4.345

Review 2.  Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.

Authors:  Shikha Kumari; Angelica V Carmona; Amit K Tiwari; Paul C Trippier
Journal:  J Med Chem       Date:  2020-08-04       Impact factor: 7.446

3.  Synthesis and SAR of a series of mGlu7 NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core.

Authors:  Jacob J Kalbfleisch; Carson W Reed; Charlotte Park; Paul K Spearing; Marc C Quitalig; Matthew T Jenkins; Alice L Rodriguez; Anna L Blobaum; P Jeffrey Conn; Colleen M Niswender; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2020-09-02       Impact factor: 2.823

Review 4.  Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental Disorders.

Authors:  Nicole M Fisher; Mabel Seto; Craig W Lindsley; Colleen M Niswender
Journal:  Front Mol Neurosci       Date:  2018-10-23       Impact factor: 5.639

5.  Corrigendum: Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental Disorders.

Authors:  Nicole M Fisher; Mabel Seto; Craig W Lindsley; Colleen M Niswender
Journal:  Front Mol Neurosci       Date:  2018-12-14       Impact factor: 5.639

6.  New 1,2,4-oxadiazole derivatives with positive mGlu4 receptor modulation activity and antipsychotic-like properties.

Authors:  Anna Stankiewicz; Katarzyna Kaczorowska; Ryszard Bugno; Aneta Kozioł; Maria H Paluchowska; Grzegorz Burnat; Barbara Chruścicka; Paulina Chorobik; Piotr Brański; Joanna M Wierońska; Beata Duszyńska; Andrzej Pilc; Andrzej J Bojarski
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.051

7.  Negative Allosteric Modulators of mGlu7 Receptor as Putative Antipsychotic Drugs.

Authors:  Paulina Cieślik; Monika Woźniak; Katarzyna Kaczorowska; Piotr Brański; Grzegorz Burnat; Agnieszka Chocyk; Bartosz Bobula; Piotr Gruca; Ewa Litwa; Agnieszka Pałucha-Poniewiera; Agnieszka Wąsik; Andrzej Pilc; Joanna Wierońska
Journal:  Front Mol Neurosci       Date:  2018-09-20       Impact factor: 5.639
  7 in total

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