title: Novel allosteric antagonists shed light on mglu(5) receptors and CNS disorders.
abstract: Although multiple metabotropic glutamate (mglu) receptor subtypes were cloned in the early 1990s, progress in the characterization of these receptors has been slow because of difficulties in obtaining subtype-selective ligands. However, in the past few years exciting progress has been made on the mglu(5) receptor subtype following the identification of selective non-amino-acid-like ligands that implicate the mglu(5) receptor as a potentially important therapeutic target, particularly for the treatment of pain and anxiety.
authors: Novartis Pharma AG, Nervous System Research, CH-4002 Basel, Switzerland. willibrordus.spooren@pharma.novartis.com
authors: W P
authors: WP
authors: Spooren
authors: F
authors: F
authors: Gasparini
authors: T E
authors: TE
authors: Salt
authors: R
authors: R
authors: Kuhn
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects / Q000502:physiology; D000818:Animals; D001007:Anxiety / Q000188:drug therapy*; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002493:Central Nervous System Diseases / Q000188:drug therapy; D003863:Depression / Q000188:drug therapy; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D009475:Neurons, Afferent / Q000187:drug effects / Q000378:metabolism; D010146:Pain / Q000188:drug therapy*; D010300:Parkinson Disease / Q000188:drug therapy*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors* / Q000502:physiology
chemical_list: D018691:Excitatory Amino Acid Antagonists; D011725:Pyridines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate; C121465:6-methyl-2-(phenylethynyl)pyridine