Rational Search for Betaine/GABA Transporter 1 Inhibitors─<i>In Vitro</i> Evaluation of Selected Hit Compound.

ABSTRACT: Inhibitory neurotransmission mediated by γ-aminobutyric acid (GABA) plays an important role in maintaining body homeostasis. Disturbances in GABA signaling are implicated in a multitude of neurologic and psychiatric conditions, including epilepsy, ischemia, anxiety, depression, insomnia, and mood disorders. Clinically relevant increases in GABA neurotransmitter level can be achieved by inhibition of its uptake into presynaptic neurons and surrounding glial cells, driven by GABA transporters (GAT1, BGT1, GAT2, and GAT3). Herein, we focused on the search for inhibitors of the BGT1 transporter which is understudied and for which the therapeutic potential of its inhibition is partly unknown. We applied multilevel virtual screening to identify compounds with inhibitory properties. Among selecte

SUBMITTER: Latka K 

PROVIDER: S-EPMC11587516 | biostudies-literature | 2024 Nov

REPOSITORIES: biostudies-literature