Receptors, Metabotropic Glutamate - Antagonists & inhibitors
Research News and Information

Monday, November 23, 2009

Interoceptive effects of alcohol require mGlu5 receptor activity in the nucleus accumbens.

27 Jul 2009 The interoceptive effects of alcohol are major determinants of addiction liability. Metabotropic glutamate (mGlu) receptors are widely expressed in striatal circuits known to modulate drug-seeking. Given that the interoceptive effects of drugs can ... Read more...

Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.

21 Jul 2009 We describe the synthesis and SAR of a series of analogues of the mGlu(5) partial antagonist 5-(phenylethynyl)pyrimidine. New molecular switches are identified that modulate the pharmacological activity of the lead compound. Slight structural ... Read more...

Effects of glutamate and alpha2-noradrenergic receptor antagonists on the development of neurotoxicity produced by chronic rotenone in rats.

15 Jul 2009 Systemic inhibition of complex I by rotenone in rats represents a model of Parkinson's disease (PD). The aim of this study was to elucidate whether neramexane (NMDA, nicotinic alpha9/alpha10 and 5-HT3 receptor antagonist), idazoxan ... Read more...

Latest indexed articles for 'Receptors, Metabotropic Glutamate - Antagonists & inhibitors'

These are the very latest articles for this heading:

• Interoceptive effects of alcohol require mGlu5 receptor activity in the nucleus accumbens. 27 Jul 2009
• Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines. 21 Jul 2009
• Effects of glutamate and alpha2-noradrenergic receptor antagonists on the development of neurotoxicity produced by chronic rotenone in rats. 15 Jul 2009
• [Effects of NMDA and metabotropic glutamate receptors antagonists in working memory task in rats] 29 Jun 2009
• Novel mGluR- and CB1R-independent suppression of GABA release caused by a contaminant of the group I metabotropic glutamate receptor agonist, DHPG. 29 Jun 2009
• Mutagenesis and molecular modeling of the orthosteric binding site of the mGlu2 receptor determining interactions of the group II receptor antagonist (3)H-HYDIA. 29 Jun 2009
• Role of the metabotropic glutamate receptor subtype 1 in the harmaline-induced tremor in rats. 22 Jun 2009
• Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1. 21 Jun 2009
• Chronic, systemic treatment with a metabotropic glutamate receptor 5 antagonist in 6-hydroxydopamine partially lesioned rats reverses abnormal firing of dopaminergic neurons. 19 Jun 2009
• Neuroprotective effects of group II metabotropic glutamate receptor agonist DCG-IV on hippocampal neurons in transient forebrain ischemia. 19 Jun 2009
• Correlation of receptor occupancy of metabotropic glutamate receptor subtype 1 (mGluR1) in mouse brain with in vivo activity of allosteric mGluR1 antagonists. 17 Jun 2009
• Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. 9 Jun 2009
• Excitatory actions of noradrenaline and metabotropic glutamate receptor activation in granule cells of the accessory olfactory bulb. 25 May 2009
• Subthreshold glutamate release from mitral cell dendrites. 25 May 2009
• A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and symptoms in gastro-oesophageal reflux disease. 18 May 2009
• Mobilization of calcium from intracellular stores facilitates somatodendritic dopamine release. 18 May 2009
• Converging signal on ERK1/2 activity regulates group I mGluR-mediated Arc transcription. 12 May 2009
• Activation of mGlu2/3 metabotropic glutamate receptors negatively regulates the stimulation of inositol phospholipid hydrolysis mediated by 5-hydroxytryptamine2A serotonin receptors in the frontal cortex of living mice. 11 May 2009
• Metabotropic glutamate receptor 5 in conditioned taste aversion learning. 7 May 2009
• Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype. May 2009

See a longer list of these articles.

Technical information about 'Receptors, Metabotropic Glutamate'

Definition: Cell surface proteins that bind glutamate and act through G-proteins to influence second messenger systems. Several types of metabotropic glutamate receptors have been cloned. They differ in pharmacology, distribution, and mechanisms of action.

Registry Number: 0

Descriptor UI: D018094

Alternative terms: Receptors, Metabotropic Glutamate; Glutamate Receptors, Metabotropic; Receptors, Glutamate, Metabotropic; Metabotropic Glutamate Receptor; Glutamate Receptor, Metabotropic; Receptor, Metabotropic Glutamate; Metabotropic Glutamate Receptors;

Allowable Qualifiers: administration & dosage; analysis; antagonists & inhibitors; biosynthesis; blood; classification; deficiency; drug effects; genetics; history; immunology; isolation & purification; metabolism; physiology; radiation effects; therapeutic use; ultrastructure; chemistry; agonists;

Tree Number: D12.776.543.750.100.450; D12.776.543.750.720.200.450.500;

History Note: 94

Technical Notes: metabotropic refers to action via the second messenger system; DF: RECEPT METAB GLUTAMATE