6533b86efe1ef96bd12cbf70

RESEARCH PRODUCT

Modulation of voltage-gated K(+) channels Kv11 and Kv1 4 by forskolin.

Gerald SeifertS. ReinhardtKatja MatthiasChristian Steinhäuser

subject

Patch-Clamp TechniquesPotassium ChannelsStereochemistryBiologyMembrane PotentialsCellular and Molecular Neurosciencechemistry.chemical_compoundmedicineCyclic AMPHumansPatch clampPhosphorylationProtein kinase ACells CulturedPharmacologyFrequency-shift keyingForskolinDose-Response Relationship DrugHEK 293 cellsColforsinCyclic AMP-Dependent Protein KinasesElectrophysiologyElectrophysiologyKineticsMechanism of actionchemistryPotassium Channels Voltage-GatedBiophysicsPhosphorylationKv1.4 Potassium Channelmedicine.symptomKv1.1 Potassium ChannelIon Channel GatingAlgorithms

description

Forskolin (FSK) affects voltage-gated K + (Kv) currents in different cell types, but it is not known which of the various subunits form FSK-sensitive Kv channels. We compared the effect of the compound at Kv1.1 and Kv1.4 channels ectopically expressed in HEK 293 cells. Low FSK concentrations induced a phosphorylation-dependent potentiation of Kv1.1 currents. At higher concentrations, this effect was superimposed by a fast, cAMP-independent channel block. Kv1.4 currents were inhibited with lower potency by FSK but were not modified by phosphorylation. The variable effect of the compound might help to distinguish between Kv subunits expressed by native cells.  2002 Elsevier Science Ltd. All rights reserved.

10.1016/s0028-3908(02)00115-6https://pubmed.ncbi.nlm.nih.gov/12243774