Literature DB >> 16115767

Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.

Peter C Chua1, Johnny Y Nagasawa, Leo S Bleicher, Benito Munoz, Edwin J Schweiger, Lida Tehrani, Jeffrey J Anderson, Merryl Cramer, Janice Chung, Mitchell D Green, Chris D King, Grace Reyes-Manalo, Nicholas D P Cosford.   

Abstract

Structure-activity relationship studies leading to the discovery of novel mGlu5 receptor antagonists are described. These compounds show high in vitro potency, have good in vivo receptor occupancy, and a reasonable intravenous pharmacokinetic profile.

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Year:  2005        PMID： 16115767     DOI： 10.1016/j.bmcl.2005.06.099

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


  2 in total

1.  Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam().

Authors:  Moses G Gichinga; Jeremy P Olson; Elizabeth Butala; Hernán A Navarro; Brian P Gilmour; S Wayne Mascarella; F Ivy Carroll
Journal:  ACS Med Chem Lett       Date:  2011-10-05       Impact factor: 4.345

2.  Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.

Authors:  Karen J Gregory; Meredith J Noetzel; Jerri M Rook; Paige N Vinson; Shaun R Stauffer; Alice L Rodriguez; Kyle A Emmitte; Ya Zhou; Aspen C Chun; Andrew S Felts; Brian A Chauder; Craig W Lindsley; Colleen M Niswender; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2012-08-03       Impact factor: 4.436
  2 in total

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