title: [Acid-Sensing Ion Channels (ASICs) in pain].
abstract: The discovery of new drug targets represents a real opportunity for developing fresh strategies against pain. Ion channels are interesting targets because they are directly involved in the detection and the transmission of noxious stimuli by sensory fibres of the peripheral nervous system and by neurons of the spinal cord. Acid-Sensing Ion Channels (ASICs) have emerged as important players in the pain pathway. They are neuronal, voltage-independent depolarizing sodium channels activated by extracellular protons. The ASIC family comprises several subunits that need to associate into homo- or hetero-trimers to form a functional channel. The ASIC1 and ASIC3 isoforms are particularly important in sensory neurons, whereas ASIC1a, alone or in association with ASIC2, is essential in the central nervous system. The potent analgesic effects associated with their inhibition in animals (which can be comparable to those of morphine) and data suggesting a role in human pain illustrate the therapeutic potential of these channels.
authors.affiliation: CNRS, Institut de Pharmacologie Moléculaire et Cellulaire, UMR 7275, 660 route des Lucioles, Sophia Antipolis, 06560 Valbonne, France - Université de Nice-Sophia Antipolis, 660 route des Lucioles, 06560 Valbonne, France - LabEx Ion Channel Science and Therapeutics, 06560 Valbonne, France.
authors.forename: Eric
authors.initials: E
authors.lastname: Lingueglia
mesh_terms: D062646:Acid Sensing Ion Channel Blockers / Q000494:pharmacology; D062565:Acid Sensing Ion Channels / Q000737:chemistry / Q000187:drug effects / Q000502:physiology*; D000200:Action Potentials / Q000502:physiology; D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D002490:Central Nervous System / Q000737:chemistry / Q000503:physiopathology; D015195:Drug Design; D045604:Extracellular Fluid / Q000737:chemistry; D006801:Humans; D006863:Hydrogen-Ion Concentration; D017136:Ion Transport; D058990:Molecular Targeted Therapy; D036421:Nerve Fibers, Unmyelinated / Q000737:chemistry / Q000502:physiology; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000502:physiology*; D059225:Nociception / Q000187:drug effects / Q000502:physiology*; D009619:Nociceptors / Q000737:chemistry / Q000187:drug effects / Q000502:physiology*; D010146:Pain / Q000503:physiopathology*; D020033:Protein Isoforms / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000502:physiology; D011984:Sensory Receptor Cells / Q000737:chemistry / Q000502:physiology; D012964:Sodium / Q000378:metabolism; D014781:Viscera / Q000294:innervation; D059265:Visceral Pain / Q000503:physiopathology
chemical_list: D062646:Acid Sensing Ion Channel Blockers; D062565:Acid Sensing Ion Channels; D000700:Analgesics; D009419:Nerve Tissue Proteins; D020033:Protein Isoforms; D012964:Sodium