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Vol. 57, Issue 5, 906-912, May 2000
Institut de Pharmacologie Moléculaire et Cellulaire, Centre
National de la Recherche Scientifique, Valbonne, France
Riluzole (RP 54274) is a potent neuroprotective agent with
anticonvulsant, sedative, and anti-ischemic properties. It is currently used in the treatment of amyotrophic lateral sclerosis. This article reports that riluzole is an activator of TREK-1 and TRAAK, two important members of a new structural family of mammalian background K+ channels with four transmembrane domains and two pore
regions. Whereas riluzole activation of TRAAK is sustained, activation of TREK-1 is transient and is followed by an inhibition. The inhibitory process is attributable to an increase of the intracellular cAMP concentration by riluzole that produces a protein kinase A-dependent inhibition of TREK-1. Mutants of TREK-1 lacking the Ser residue where
the kinase A phosphorylation takes place are activated in a sustained
manner by riluzole. TRAAK is permanently activated by riluzole because,
unlike TREK-1, it lacks the negative regulation by cAMP.
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