title: Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists.
abstract: Modulation of the metabotropic glutamate subtype 5 (mGlu5) receptor may be useful in the treatment of a variety of central nervous system disorders. Herein, we report on the discovery, synthesis, and biological evaluation of dipyridyl amines as small molecule mGlu5 antagonists.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA. kameneck@scripps.edu
authors.forename: Theodore M
authors.initials: TM
authors.lastname: Kamenecka
authors.forename: Céline
authors.initials: C
authors.lastname: Bonnefous
authors.forename: Steven
authors.initials: S
authors.lastname: Govek
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Vernier
authors.forename: John
authors.initials: J
authors.lastname: Hutchinson
authors.forename: Janice
authors.initials: J
authors.lastname: Chung
authors.forename: Grace
authors.initials: G
authors.lastname: Reyes-Manalo
authors.forename: Jeffery J
authors.initials: JJ
authors.lastname: Anderson
mesh_terms: D000588:Amines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D010599:Pharmacokinetics; D011725:Pyridines / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D018691:Excitatory Amino Acid Antagonists; D011725:Pyridines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate