title: Targeting α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate receptors in epilepsy.
abstract: BACKGROUND
  Despite epilepsies being between the oldest and most studied neurological diseases, new treatment remains an unmet need of scientific research due to the high percentage of refractory patients. Several studies have identified new suitable anti-seizure targets. Glutamate activation of α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate receptors (AMPARs) have long ago been identified as suitable targets for the development of anti seizure drugs.
  
  
  METHODS
  Here, we describe: i) AMPARs' structure and their involvement and role during seizures and in epilepsy and ii) the efficacy of AMPAR antagonists in preclinical models of seizures and epilepsy.
  
  
  CONCLUSIONS
  The physiological and pathological role of AMPAR in the CNS and the development of AMPAR antagonists have recently gained attention considering their recent involvement in status epilepticus and the marketing of perampanel. The need for new anti-seizure drugs represents a major challenge in both preclinical and clinical epilepsy. The introduction into the market of perampanel for the treatment of epilepsy will shed new light on the real potential of AMPAR antagonism in clinical settings outside the limited world of clinical trials. While research will go on in this area, fundamental will be the post-marketing evaluation of perampanel efficacy and tolerability and a better definition of the role of this receptor in the epileptic brain.
authors.affiliation: University "Magna Graecia" of Catanzaro, School of Medicine, Science of Health Department , Catanzaro , Italy.
authors.forename: Rita
authors.initials: R
authors.lastname: Citraro
authors.forename: Rossana
authors.initials: R
authors.lastname: Aiello
authors.forename: Valentina
authors.initials: V
authors.lastname: Franco
authors.forename: Giovambattista
authors.initials: G
authors.lastname: De Sarro
authors.forename: Emilio
authors.initials: E
authors.lastname: Russo
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology / Q000627:therapeutic use*; D004827:Epilepsy / Q000188:drug therapy* / Q000378:metabolism; D006801:Humans; D011487:Protein Conformation; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism
chemical_list: D000927:Anticonvulsants; D018091:Receptors, AMPA