title: Flupirtine, a re-discovered drug, revisited.
abstract: Flupirtine was developed long before K(V)7 (KCNQ) channels were known. However, it was clear from the beginning that flupirtine is neither an opioid nor a nonsteroidal anti-inflammatory analgesic. Its unique muscle relaxing activity was discovered by serendipity. In the meantime, broad and intensive research has resulted in a partial clarification of its mode of action. Flupirtine is the first therapeutically used K(V)7 channel activator with additional GABA(A)ergic mechanisms and thus the first representative of a novel class of analgesics. The presently accepted main mode of its action, potassium K(V)7 (KCNQ) channel activation, opens a series of further therapeutic possibilities. One of them has now been realized: its back-up compound, the bioisostere retigabine, has been approved for the treatment of epilepsy.
authors: Institute for Experimental and Clinical Pharmacology and Toxicology, Doerenkamp-Chair for Innovations in Animal and Consumer Protection, Friedrich-Alexander University, Fahrstrasse 17, 91054 Erlangen, Germany. szelenyi@pharmakologie.uni-erlangen.de
authors: Istvan
authors: I
authors: Szelenyi
mesh_terms: D000631:Aminopyridines / Q000627:therapeutic use*; D000700:Analgesics / Q000627:therapeutic use*; D004827:Epilepsy / Q000188:drug therapy; D006801:Humans; D051656:KCNQ Potassium Channels / Q000819:agonists; D009437:Neuralgia / Q000188:drug therapy; D009465:Neuromuscular Agents / Q000627:therapeutic use*; D053201:Urinary Bladder, Overactive / Q000188:drug therapy
chemical_list: D000631:Aminopyridines; D000700:Analgesics; D051656:KCNQ Potassium Channels; D009465:Neuromuscular Agents; C034161:flupirtine