Metabotropic receptors as targets for drugs of potential use in the treatment of neuropathic pain.
Glutamate is the major neurotransmitter in the mammalian central nervous system and plays a pivotal role in both acute and chronic pain. The actions of glutamate are mediated by two receptor families: ionotropic glutamate receptors (iGluRs), and metabotropic glutamate receptors (mGluRs). Activation of glutamate receptor can elicit both hyperalgesic and analgesic effects. Eight mGluRs subtypes (mGluR1-mGluR8) have been identified and classified into three groups. Among these, group I mGluRs (mGlu1 and -5) have been implicated in the processes of central sensitization and persistent nociception, whereas activation of group II mGluRs (mGlu2/3) is effective against neuropathic or inflammatory pain. In this review we focus on the role of mGlu2/3 in the modulation of persistent pain, and on their potential use as drug targets in pain management.
Department of Pharmaceutical Science, University of Catania, Catania, Italy.
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S
Chiechio
A
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Copani
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D
Melchiorri
A M Teixido
AM
Canudas
M
M
Storto
M
M
Calvani
R
R
Nicolai
F
F
Nicoletti
D000108:Acetylcarnitine / Q000627:therapeutic use; D000700:Analgesics / Q000627:therapeutic use; D000818:Animals; D006801:Humans; D018697:Nootropic Agents / Q000627:therapeutic use; D010146:Pain / Q000188:drug therapy* / Q000209:etiology / Q000503:physiopathology; D010523:Peripheral Nervous System Diseases / Q000150:complications / Q000188:drug therapy* / Q000503:physiopathology; D018094:Receptors, Metabotropic Glutamate / Q000187:drug effects* / Q000502:physiology
D000700:Analgesics; D018697:Nootropic Agents; D018094:Receptors, Metabotropic Glutamate; C108822:metabotropic glutamate receptor 2; C102718:metabotropic glutamate receptor 3; D000108:Acetylcarnitine