title: Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
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.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2 3535 General Atomics Court, San Diego, CA 92121, USA. pchua@cylenepharma.com
authors.forename: Peter C
authors.initials: PC
authors.lastname: Chua
authors.forename: Johnny Y
authors.initials: JY
authors.lastname: Nagasawa
authors.forename: Leo S
authors.initials: LS
authors.lastname: Bleicher
authors.forename: Benito
authors.initials: B
authors.lastname: Munoz
authors.forename: Edwin J
authors.initials: EJ
authors.lastname: Schweiger
authors.forename: Lida
authors.initials: L
authors.lastname: Tehrani
authors.forename: Jeffrey J
authors.initials: JJ
authors.lastname: Anderson
authors.forename: Merryl
authors.initials: M
authors.lastname: Cramer
authors.forename: Janice
authors.initials: J
authors.lastname: Chung
authors.forename: Mitchell D
authors.initials: MD
authors.lastname: Green
authors.forename: Chris D
authors.initials: CD
authors.lastname: King
authors.forename: Grace
authors.initials: G
authors.lastname: Reyes-Manalo
authors.forename: Nicholas D P
authors.initials: ND
authors.lastname: Cosford
mesh_terms: D018691:Excitatory Amino Acid Antagonists / Q000493:pharmacokinetics / Q000494:pharmacology*; D011725:Pyridines / Q000493:pharmacokinetics / Q000494:pharmacology*; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*
chemical_list: D018691:Excitatory Amino Acid Antagonists; D011725:Pyridines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate