Novel allosteric antagonists shed light on mglu(5) receptors and CNS disorders.
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.
Spooren
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Novartis Pharma AG, Nervous System Research, CH-4002 Basel, Switzerland. willibrordus.spooren@pharma.novartis.com
Gasparini
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Salt
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Kuhn
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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
D018691:Excitatory Amino Acid Antagonists; D011725:Pyridines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate; C121465:6-methyl-2-(phenylethynyl)pyridine