title: Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain.
abstract: A series of fused tricyclic mGluR1 antagonists containing a pyridone ring were synthesized. In vitro, these antagonists were potent against both human and rat isozymes, as well as selective for inhibiting mGluR1 over mGluR5. When dosed orally, several examples were active in vivo in a rat SNL test.
authors.affiliation: Merck Research Laboratories, Kenilworth, NJ 07033-0539, USA. chadbennett3@yahoo.com
authors.forename: Chad E
authors.initials: CE
authors.lastname: Bennett
authors.forename: Duane A
authors.initials: DA
authors.lastname: Burnett
authors.forename: William J
authors.initials: WJ
authors.lastname: Greenlee
authors.forename: Chad E
authors.initials: CE
authors.lastname: Knutson
authors.forename: Peter
authors.initials: P
authors.lastname: Korakas
authors.forename: Cheng
authors.initials: C
authors.lastname: Li
authors.forename: Deen
authors.initials: D
authors.lastname: Tulshian
authors.forename: Wen-Lian
authors.initials: WL
authors.lastname: Wu
authors.forename: Rosalia
authors.initials: R
authors.lastname: Bertorelli
authors.forename: Silva
authors.initials: S
authors.lastname: Fredduzzi
authors.forename: Mariagrazia
authors.initials: M
authors.lastname: Grilli
authors.forename: Gianluca
authors.initials: G
authors.lastname: Lozza
authors.forename: Angelo
authors.initials: A
authors.lastname: Reggiani
authors.forename: Alessio
authors.initials: A
authors.lastname: Veltri
mesh_terms: D000284:Administration, Oral; D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D002478:Cells, Cultured; D003500:Cyclization; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009437:Neuralgia / Q000188:drug therapy; D011485:Protein Binding / Q000187:drug effects; D011728:Pyridones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*
chemical_list: D000700:Analgesics; D011728:Pyridones; D018094:Receptors, Metabotropic Glutamate; C104077:metabotropic glutamate receptor type 1