Chloride transporters controlling neuronal excitability

JC Pressey, M de Saint-Rome… - Physiological …, 2023 - journals.physiology.org
Synaptic inhibition plays a crucial role in regulating neuronal excitability, which is the
foundation of nervous system function. This inhibition is largely mediated by the …

Off-label use of bumetanide for brain disorders: an overview

SC Kharod, SK Kang, SD Kadam - Frontiers in neuroscience, 2019 - frontiersin.org
Bumetanide (BTN or BUM) is a FDA-approved potent loop diuretic (LD) that acts by
antagonizing sodium-potassium-chloride (Na-K-Cl) cotransporters, NKCC1 (SLc12a2) and …

Analysis of genome-wide association data highlights candidates for drug repositioning in psychiatry

HC So, CKL Chau, WT Chiu, KS Ho, CP Lo… - Nature …, 2017 - nature.com
Abstract Knowledge of psychiatric disease genetics has advanced rapidly during the past
decade with the advent of genome-wide association studies (GWAS). However, less …

Discovery of a small molecule drug candidate for selective NKCC1 inhibition in brain disorders

A Savardi, M Borgogno, R Narducci, G La Sala… - Chem, 2020 - cell.com
Aberrant expression ratio of Cl− transporters, NKCC1 and KCC2, is implicated in several
brain conditions. NKCC1 inhibition by the FDA-approved diuretic drug, bumetanide, rescues …

Evaluation of bumetanide as a potential therapeutic agent for Alzheimer's disease

B Boyarko, S Podvin, B Greenberg… - Frontiers in …, 2023 - frontiersin.org
Therapeutics discovery and development for Alzheimer's disease (AD) has been an area of
intense research to alleviate memory loss and the underlying pathogenic processes. Recent …

Cation-chloride cotransporters KCC2 and NKCC1 as therapeutic targets in neurological and neuropsychiatric disorders

P Lam, J Newland, RLM Faull, A Kwakowsky - Molecules, 2023 - mdpi.com
Neurological diseases including Alzheimer's, Huntington's disease, Parkinson's disease,
Down syndrome and epilepsy, and neuropsychiatric disorders such as schizophrenia, are …

Physiological processes modulated by the chloride-sensitive WNK-SPAK/OSR1 kinase signaling pathway and the cation-coupled chloride cotransporters

AR Murillo-de-Ozores, M Chávez-Canales… - Frontiers in …, 2020 - frontiersin.org
The role of Cl–as an intracellular signaling ion has been increasingly recognized in recent
years. One of the currently best described roles of Cl–in signaling is the modulation of the W …

Depolarizing GABAA current in the prefrontal cortex is linked with cognitive impairment in a mouse model relevant for schizophrenia

HR Kim, L Rajagopal, HY Meltzer, M Martina - Science Advances, 2021 - science.org
Cognitive impairment in schizophrenia (CIAS) is the most critical predictor of functional
outcome. Limited understanding of the cellular mechanisms of CIAS hampers development …

Succinic semialdehyde dehydrogenase deficiency, a disorder of GABA metabolism: an update on pharmacological and enzyme-replacement therapeutic strategies

KR Vogel, GR Ainslie, DC Walters, A McConnell… - Journal of inherited …, 2018 - Springer
We present an update to the status of research on succinic semialdehyde dehydrogenase
(SSADH) deficiency (SSADHD), a rare disorder of GABA metabolism. This is an unusual …

Drugs targeting APOE4 that regulate beta‐amyloid aggregation in the brain: therapeutic potential for Alzheimer's disease

J Poblano, I Castillo‐Tobías, L Berlanga… - Basic & Clinical …, 2024 - Wiley Online Library
Alzheimer's disease is characterized by progressive cognitive decline, and behavioural and
psychological symptoms of dementia are common. The APOE ε4 allele, a genetic risk factor …