2008
DOI: 10.1016/j.pharmthera.2007.09.003
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Modulation of pain transmission by G-protein-coupled receptors

Abstract: The heterotrimeric G protein-coupled receptors (GPCRs) represent the largest and most diverse family of cell surface receptors and proteins. GPCRs are widely distributed in the peripheral and central nervous systems and are one of the most important therapeutic targets in pain medicine. GPCRs are present on the plasma membrane of neurons and their terminals along the nociceptive pathways and are closely associated with the modulation of pain transmission. GPCRs that can produce analgesia upon activation includ… Show more

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Cited by 169 publications
(130 citation statements)
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References 316 publications
(386 reference statements)
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“…many G i/o -coupled receptors (21). Interestingly, stimulation of mAChRs potentiates glutamate release in the majority of spinal dorsal horn neurons in mice (22), which makes it difficult to explain the analgesic effect of mAChR agonists and acetylcholinesterase inhibitors.…”
mentioning
confidence: 99%
“…many G i/o -coupled receptors (21). Interestingly, stimulation of mAChRs potentiates glutamate release in the majority of spinal dorsal horn neurons in mice (22), which makes it difficult to explain the analgesic effect of mAChR agonists and acetylcholinesterase inhibitors.…”
mentioning
confidence: 99%
“…The conduction of peripheral pain signals involves glutamate receptors. [60][61][62][63][64] Calcitonin-gene related peptide and substance P are entangled in the disinhibition of the ionotropic-glutamate NMDA receptors. Moreover, metabotropic-glutamate receptors hinder the adenylyl-cyclase and decreases the conduction of pain signals.…”
Section: Sensitization Of Nociceptorsmentioning
confidence: 99%
“…[19,20,21,22] While the mechanism and location of action of the sedative effect of these compounds are due to the hyperpolarization of excitable neurons localized in the nucleous coereleus, the analgesic effect of these drugs is not completely understood, and have a complex mechanism. Alpha 2 agonists induce analgesia by acting in different places; brain, brain stem, spinal cord and peripheral nerves.…”
Section: Topics In Spinal Anaesthesia 100mentioning
confidence: 99%