title: Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): efficacy in an animal model for schizophrenia.
abstract: Metabotropic glutamate receptor 2 (mGluR2) has been implicated in a variety of CNS disorders, including schizophrenia. Disclosed herein is the development of a new series of allosteric potentiators of mGluR2. Structure-activity relationship studies in conjunction with pharmacokinetic data led to the discovery of indole 5, which is active in an animal model for schizophrenia.
authors: Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA. sgovek@san.rr.com
authors: Steven P
authors: SP
authors: Govek
authors: Celine
authors: C
authors: Bonnefous
authors: John H
authors: JH
authors: Hutchinson
authors: Theodore
authors: T
authors: Kamenecka
authors: Jeffrey
authors: J
authors: McQuiston
authors: Richard
authors: R
authors: Pracitto
authors: Lucy X
authors: LX
authors: Zhao
authors: Michael F
authors: MF
authors: Gardner
authors: Joyce K
authors: JK
authors: James
authors: Lorrie P
authors: LP
authors: Daggett
authors: Blake A
authors: BA
authors: Rowe
authors: Hervé
authors: H
authors: Schaffhauser
authors: Linda J
authors: LJ
authors: Bristow
authors: Una C
authors: UC
authors: Campbell
authors: Dana E
authors: DE
authors: Rodriguez
authors: Jean-Michel
authors: JM
authors: Vernier
mesh_terms: D000098:Acetophenones / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000494:Allosteric Regulation / Q000187:drug effects; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D003432:Cross-Linking Reagents / Q000737:chemistry; D004195:Disease Models, Animal; D006801:Humans; D007649:Ketamine / Q000494:pharmacology; D015394:Molecular Structure; D051381:Rats; D018094:Receptors, Metabotropic Glutamate / Q000378:metabolism*; D012559:Schizophrenia / Q000139:chemically induced / Q000188:drug therapy* / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D000098:Acetophenones; D003432:Cross-Linking Reagents; D018094:Receptors, Metabotropic Glutamate; C108822:metabotropic glutamate receptor 2; D007649:Ketamine