GABAA receptors: structure, function, pharmacology, and related disorders

A Ghit, D Assal, AS Al-Shami, DEE Hussein - Journal of Genetic …, 2021 - Springer
Background γ-Aminobutyric acid sub-type A receptors (GABAARs) are the most prominent
inhibitory neurotransmitter receptors in the CNS. They are a family of ligand-gated ion …

Understanding the mechanism of action and clinical effects of neuroactive steroids and GABAergic compounds in major depressive disorder

AJ Cutler, GW Mattingly, V Maletic - Translational Psychiatry, 2023 - nature.com
The pathophysiology of major depressive disorder (MDD) is thought to result from impaired
connectivity between key brain networks. Gamma-aminobutyric acid (GABA) is the key …

GABAkines–Advances in the discovery, development, and commercialization of positive allosteric modulators of GABAA receptors

A Lippa, MM Poe, JL Smith, X Jin, X Ping… - Pharmacology & …, 2022 - Elsevier
Positive allosteric modulators of γ-aminobutyric acid-A (GABA A) receptors or GABAkines
have been widely used medicines for over 70 years for anxiety, epilepsy, sleep, and other …

Knockdown of GABAA alpha3 subunits on thalamic reticular neurons enhances deep sleep in mice

DS Uygun, C Yang, ER Tilli, F Katsuki… - Nature …, 2022 - nature.com
Identification of mechanisms which increase deep sleep could lead to novel treatments
which promote the restorative effects of sleep. Here, we show that knockdown of the α3 …

Significance of GABAA Receptor for Cognitive Function and Hippocampal Pathology

Y Sakimoto, PMT Oo, M Goshima, I Kanehisa… - International Journal of …, 2021 - mdpi.com
The hippocampus is a primary area for contextual memory, known to process spatiotemporal
information within a specific episode. Long-term strengthening of glutamatergic transmission …

In vivo‐and in silico‐driven identification of novel synthetic quinoxalines as anticonvulsants and AMPA inhibitors

HS Abulkhair, S Elmeligie, A Ghiaty… - Archiv der …, 2021 - Wiley Online Library
The lack of effective therapies for epileptic patients and the potentially harmful
consequences of untreated seizure incidents have made epileptic disorders in humans a …

Anti-apoptotic actions of allopregnanolone and ganaxolone mediated through membrane progesterone receptors (PAQRs) in neuronal cells

P Thomas, Y Pang - Frontiers in endocrinology, 2020 - frontiersin.org
The neurosteroids progesterone and allopregnanolone regulate numerous neuroprotective
functions in neural tissues including inhibition of epileptic seizures and cell death. Many of …

Mechanistic and therapeutic relationships of traumatic brain injury and γ-amino-butyric acid (GABA)

JM Witkin, H Shafique, JL Smith, AM Marini… - Pharmacology & …, 2024 - Elsevier
Traumatic brain injury is a highly prevalent medical condition for which no medications
specific for the prophylaxis or treatment of the condition as a whole exist. The spectrum of …

Drug development in channelopathies: Allosteric modulation of ligand-gated and voltage-gated ion channels

Y Zhang, K Wang, Z Yu - Journal of medicinal chemistry, 2020 - ACS Publications
Ion channels have been characterized as promising drug targets for treatment of numerous
human diseases. Functions of ion channels can be fine-tuned by allosteric modulators …

Recent progress in the development of new antiepileptic drugs with novel targets

TM Belete - Annals of Neurosciences, 2023 - journals.sagepub.com
Background Epilepsy is a chronic neurological disorder that affects approximately 50–70
million people worldwide. Epilepsy has a significant economic and social burden on patients …