The new anticonvulsant retigabine (D-23129) acts as an opener of K + channels in neuronal cells

The new anticonvulsant retigabine (D-23129) acts as an opener of K + channels in neuronal cells The patch clamp technique was used to measure currents passing through K + channels in neuronal cell preparations. Retigabine (D-23129, N -(2-amino-4-(4-fluorobenzylamino)-phenyl) carbamic acid ethyl ester) activated a K + conductance in slightly depolarized NG108-15 neuronal cells in a dose dependent manner (0.1–10 μ M). At the K + reversal potential, no current could be elicited and in hyperpolarized cells the current was reversed. A similar current was elicited in primary cultures of mouse cortical neurones and in differentiated hNT cells, a cell line derived from human neuronal cells. At higher concentrations, retigabine also partially blocked voltage activated K + currents. None of the tested anticonvulsants, phenytoin, carbamazepine and valproate and none of the K + channel openers cromakalim, diazoxide and pinacidil exerted a similar effect. The current was not affected by the K + channel blocker glibenclamide (10 μ M) but was fully blocked by application of Ba 2+ (10.8 mM). Exchange of K + with cesium in the intracellular space also fully abolished the current. It can be expected that the K + channel opening effect contributes to the anticonvulsant activity of retigabine. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png European Journal of Pharmacology Elsevier

The new anticonvulsant retigabine (D-23129) acts as an opener of K + channels in neuronal cells

European Journal of Pharmacology, Volume 336 (2) – Oct 8, 1997

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Publisher
Elsevier
Copyright
Copyright © 1997 Elsevier Science B.V.
ISSN
0014-2999
DOI
10.1016/S0014-2999(97)01249-1
Publisher site
See Article on Publisher Site

Abstract

The patch clamp technique was used to measure currents passing through K + channels in neuronal cell preparations. Retigabine (D-23129, N -(2-amino-4-(4-fluorobenzylamino)-phenyl) carbamic acid ethyl ester) activated a K + conductance in slightly depolarized NG108-15 neuronal cells in a dose dependent manner (0.1–10 μ M). At the K + reversal potential, no current could be elicited and in hyperpolarized cells the current was reversed. A similar current was elicited in primary cultures of mouse cortical neurones and in differentiated hNT cells, a cell line derived from human neuronal cells. At higher concentrations, retigabine also partially blocked voltage activated K + currents. None of the tested anticonvulsants, phenytoin, carbamazepine and valproate and none of the K + channel openers cromakalim, diazoxide and pinacidil exerted a similar effect. The current was not affected by the K + channel blocker glibenclamide (10 μ M) but was fully blocked by application of Ba 2+ (10.8 mM). Exchange of K + with cesium in the intracellular space also fully abolished the current. It can be expected that the K + channel opening effect contributes to the anticonvulsant activity of retigabine.

Journal

European Journal of PharmacologyElsevier

Published: Oct 8, 1997

References

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