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Flupirtine, a re-discovered drug, revisited.
MedLine Citation:
PMID:  23322112     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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:
Istvan Szelenyi
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-1-16
Journal Detail:
Title:  Inflammation research : official journal of the European Histamine Research Society ... [et al.]     Volume:  -     ISSN:  1420-908X     ISO Abbreviation:  Inflamm. Res.     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-1-16     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9508160     Medline TA:  Inflamm Res     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
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.
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