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Retigabine (D-23129)
English articles
Research & Development
Retigabine (D-23129)
| Retigabine (D-23129) |
Retigabine, a anticonvulsant, known already sinds 1995, activates Kv7 (KCNQ/M) channels in the axonal/nodal membrane of peripheral myelinated axons.
Retigabine for neuropathic pain?Retigabine influences the excitability parameters of C-type nerve fibers in a paradigm based on isolated fascicles of human sural nerve. Application of retigabine (3-10 microM) produced an increase in membrane threshold, and this points out that retigabine produces a membrane hyperpolarization which is limited by the K(+) equilibrium potential. Kv7 channels are present on axons of unmyelinated, including nociceptive, peripheral human nerve fibers. It is likely that the affinity of retigabine for these channels may reduce the ectopic generation of action potentials in neuropathic pain, and thus making retigabine a novel candidate neuropathic analgesic drug. [1] [2] June 2010, Jan M. Keppel Hesselink, MD, PhD Referenties[1]: Lang PM, Fleckenstein J, Passmore GM, Brown DA, Grafe P. | Retigabine reduces the excitability of unmyelinated peripheral human axons. | Neuropharmacology. | 2008 Jun;54(8):1271-8. Epub 2008 Apr 18. [2]: Blackburn-Munro G, Jensen BS. | The anticonvulsant retigabine attenuates nociceptive behaviours in rat models of persistent and neuropathic pain. | Eur J Pharmacol. | 2003 Jan 24;460(2-3):109-16. |
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