• Inflamm. Res. · Mar 2013

    Review

    Flupirtine, a re-discovered drug, revisited.

    • Istvan Szelenyi.
    • 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
    • Inflamm. Res. 2013 Mar 1; 62 (3): 251-8.

    AbstractFlupirtine 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.

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