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..
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2013 |
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| Erschienen: |
2013 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:62 |
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| Enthalten in: |
Inflammation research - 62(2013), 3 vom: 16. Jan., Seite 251-258 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Szelenyi, Istvan [VerfasserIn] |
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| Links: |
Volltext [lizenzpflichtig] |
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| Themen: |
Analgesia |
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| Anmerkungen: |
© Springer Basel 2013 |
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| doi: |
10.1007/s00011-013-0592-5 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a 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. | ||
| 650 | 4 | |a Analgesia | |
| 650 | 4 | |a Skeletal muscle relaxation | |
| 650 | 4 | |a Potassium channels | |
| 650 | 4 | |a GABA | |
| 650 | 4 | |a Retigabine | |
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| 952 | |d 62 |j 2013 |e 3 |b 16 |c 01 |h 251-258 | ||