Literature DB >> 19289283

In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.

Simon J Mantell1, Karl R Gibson, Simon A Osborne, Graham N Maw, Huw Rees, Peter G Dodd, Ben Greener, Gareth W Harbottle, William A Million, Cedric Poinsard, Steven England, Pauline Carnell, Alison M Betts, Russell Monhemius, Rebecca L Prime.   

Abstract

The SAR of a series of novel pyrido[3,4-d]pyramid-4-ylamine mGluR1 antagonists is described. The multiple of the unbound K(i) in cerebrospinal fluid necessary to give morphine like analgesic effects in an electromyograph pinch model in rodents is determined and the effect of structure on CNS penetration examined.

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Year:  2009        PMID： 19289283     DOI： 10.1016/j.bmcl.2009.02.106

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

Review 1.  Recent advances in the medicinal chemistry of the metabotropic glutamate receptor 1 (mGlu₁).

Authors:  Dafydd R Owen
Journal:  ACS Chem Neurosci       Date:  2011-03-10       Impact factor: 4.418

2.  A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors.

Authors:  Hyekyung P Cho; Darren W Engers; Daryl F Venable; Colleen M Niswender; Craig W Lindsley; P Jeffrey Conn; Kyle A Emmitte; Alice L Rodriguez
Journal:  ACS Chem Neurosci       Date:  2014-05-15       Impact factor: 4.418

3.  N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents.

Authors:  Andrew S Felts; Alice L Rodriguez; Ryan D Morrison; Daryl F Venable; Anna L Blobaum; Frank W Byers; J Scott Daniels; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2016-03-09       Impact factor: 2.823

4.  Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.

Authors:  Andrew S Felts; Sam A Saleh; Uyen Le; Alice L Rodriguez; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2009-10-09       Impact factor: 2.823

5.  Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.

Authors:  Jason T Manka; Alice L Rodriguez; Ryan D Morrison; Daryl F Venable; Hyekyung P Cho; Anna L Blobaum; J Scott Daniels; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2013-07-23       Impact factor: 2.823

6.  N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.

Authors:  Kimberly M Lovell; Andrew S Felts; Alice L Rodriguez; Daryl F Venable; Hyekyung P Cho; Ryan D Morrison; Frank W Byers; J Scott Daniels; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2013-05-17       Impact factor: 2.823
  6 in total

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