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Pharmacology and functions of metabotropic glutamate receptors.

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TLDR
The findings suggest that the mGluRs provide a novel target for development of therepeutic agents that could have a significant impact on neuropharmacology.
Abstract
▪ Abstract In the mid to late 1980s, studies were published that provided the first evidence for the existence of glutamate receptors that are not ligand-gated cation channels but are coupled to effector systems through GTP-binding proteins. Since those initial reports, tremendous progress has been made in characterizing these metabotropic glutamate receptors (mGluRs), including cloning and characterization of cDNA that encodes a family of eight mGluR subtypes, several of which have multiple splice variants. Also, tremendous progress has been made in developing new highly selective mGluR agonists and antagonists and toward determining the physiologic roles of the mGluRs in mammalian brain. These findings have exciting implications for drug development and suggest that the mGluRs provide a novel target for development of therepeutic agents that could have a significant impact on neuropharmacology.

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Citations
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Central Sensitization: A Generator of Pain Hypersensitivity by Central Neural Plasticity

TL;DR: The major triggers that initiate and maintain central sensitization in healthy individuals in response to nociceptor input and in patients with inflammatory and neuropathic pain are reviewed, emphasizing the fundamental contribution and multiple mechanisms of synaptic plasticity caused by changes in the density, nature, and properties of ionotropic and metabotropic glutamate receptors.
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Descending control of pain.

TL;DR: The present review focuses on the organisation of descending pathways and their pathophysiological significance, the role of individual transmitters and specific receptor types in the modulation and expression of mechanisms of descending inhibition and facilitation and the advantages and limitations of established and innovative analgesic strategies which act by manipulation of descending controls.
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The induction of pain: an integrative review

TL;DR: A global account of mechanisms involved in the induction of pain is provided, including neuronal pathways for the transmission of nociceptive information from peripheral nerve terminals to the dorsal horn, and therefrom to higher centres.
Journal ArticleDOI

Metabotropic Glutamate Receptors: Physiology, Pharmacology, and Disease

TL;DR: The widespread expression of mGluRs makes these receptors particularly attractive drug targets, and recent studies continue to validate the therapeutic utility of m GluR ligands in neurological and psychiatric disorders such as Alzheimer's disease, Parkinson's Disease, anxiety, depression, and schizophrenia.
Journal ArticleDOI

Glutamate as a Neurotransmitter in the Brain: Review of Physiology and Pathology

TL;DR: Endogenous glutamate, by activating NMDA, AMPA or mGluR1 receptors, may contribute to the brain damage occurring acutely after status epilepticus, cerebral ischemia or traumatic brain injury, and may also contribute to chronic neurodegeneration in such disorders as amyotrophic lateral sclerosis and Huntington's chorea.
References
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Journal ArticleDOI

Cloned Glutamate Receptors

TL;DR: The application of molecular cloning technology to the study of the glutamate receptor system has led to an explosion of knowledge about the structure, expression, and function of this most important fast excitatory transmitter system in the mammalian brain.
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Molecular diversity of glutamate receptors and implications for brain function.

TL;DR: The molecular and functional diversity of the glutamate receptors is reviewed and their implications for integrative brain function are discussed.
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Cloning and characterization of an extracellular Ca 2+ -sensing receptor from bovine parathyroid

TL;DR: The cloning of complementary DNA encoding an extracellular Ca2+ -sensing receptor from bovine parathyroid is reported with pharmacological and functional properties nearly identical to those of the native receptor.
Journal ArticleDOI

The metabotropic glutamate receptors: structure and functions.

TL;DR: Recently, glutamate has been shown to regulate ion channels and enzymes producing second messengers via specific receptors coupled to G-proteins, and the existence of these receptors is changing views on the functioning of fast excitatory synapses.
Journal ArticleDOI

Sequence and expression of a metabotropic glutamate receptor

TL;DR: The complementary DNA of a metabotropic glutamate receptor coupled to inositol phosphate/Ca2+ signal transduction has been cloned and characterized and abundant expression of this messenger RNA is observed in neuronal cells in hippocampal dentate gyrus and CA2−3 and in Cerebellar Purkinje cells, suggesting the importance of this receptor in specific hippocampal and cerebellar functions.
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