Assay Method Information

Assay Name:  Identification of Novel Modulators of Cl- dependent Transport Process via HTS; Dose-dependent Assay with KCC2
Description:  Vanderbilt Screening Center for GPCRs, Ion Channels and Transporters Assay Provider: Eric Delpire Assay Provider Affliation: Vanderbilt University Grant Title: Identification of Novel Modulators of Cl- dependent Transport Process via HTS Grant Number: R21NS053658-01 Cation-chloride cotransporters such as K-Cl cotransport and Na-K-2Cl cotransport play major roles in a variety of physiological settings, including the modulation of GABAergic synaptic transmission. For instance, KCC2, a neuronal-specific K-Cl cotransporter is up-regulated in the brain during postnatal development, and is responsible for lowering the intracellular Cl- concentration in neurons, thus promoting GABA inhibition. Reduction in KCC2 expression results in brain hyperexcitability, as demonstrated by animal models. Furthermore, KCC2 expression is decreased in brain tissue isolated from epileptic patients. There are very few pharmacological agents that affect K-Cl cotransporters. First, there are no specific inhibi
Affinity data for this assay
 

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