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Flupirtine, a re-discovered drug, revisited

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Abstract

Flupirtine was developed long before KV7 (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 KV7 channel activator with additional GABAAergic mechanisms and thus the first representative of a novel class of analgesics. The presently accepted main mode of its action, potassium KV7 (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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Acknowledgments

I am grateful to Dr Berthold Renner for valuable and constructive comments and helpful discussions.

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  1. 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

    Istvan Szelenyi

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Szelenyi, I. Flupirtine, a re-discovered drug, revisited. Inflamm. Res. 62, 251–258 (2013). https://doi.org/10.1007/s00011-013-0592-5

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