Structure, function, and modulation of GABAA receptors

E Sigel, ME Steinmann - Journal of Biological Chemistry, 2012 - ASBMB
The GABA A receptors are the major inhibitory neurotransmitter receptors in mammalian
brain. Each isoform consists of five homologous or identical subunits surrounding a central …

The benzodiazepine binding sites of GABAA receptors

E Sigel, M Ernst - Trends in pharmacological sciences, 2018 - cell.com
Everyday activity is based on a subtle equilibrium of excitatory and inhibitory neuronal
systems. The most prominent players in neuronal inhibition are synaptic and extrasynaptic …

Structure of a human synaptic GABAA receptor

S Zhu, CM Noviello, J Teng, RM Walsh Jr, JJ Kim… - Nature, 2018 - nature.com
Fast inhibitory neurotransmission in the brain is principally mediated by the neurotransmitter
GABA (γ-aminobutyric acid) and its synaptic target, the type A GABA receptor (GABAA …

Why won't it stop? The dynamics of benzodiazepine resistance in status epilepticus

RJ Burman, RE Rosch, JM Wilmshurst, A Sen… - Nature Reviews …, 2022 - nature.com
Status epilepticus is a life-threatening neurological emergency that affects both adults and
children. Approximately 36% of episodes of status epilepticus do not respond to the current …

International Union of Basic and Clinical Pharmacology. CVI: GABAA receptor subtype-and function-selective ligands: key issues in translation to humans

W Sieghart, MM Savić - Pharmacological reviews, 2018 - ASPET
GABAA receptors are the major inhibitory transmitter receptors in the brain. They are ligand-
gated chloride channels and the site of action of benzodiazepines, barbiturates, neuroactive …

Docking screens for novel ligands conferring new biology: Miniperspective

JJ Irwin, BK Shoichet - Journal of medicinal chemistry, 2016 - ACS Publications
It is now plausible to dock libraries of 10 million molecules against targets over several days
or weeks. When the molecules screened are commercially available, they may be rapidly …

[HTML][HTML] Patterns of mRNA and protein expression for 12 GABAA receptor subunits in the mouse brain

H Hörtnagl, RO Tasan, A Wieselthaler, E Kirchmair… - Neuroscience, 2013 - Elsevier
The GABAA receptor is the main inhibitory receptor in the brain and its subunits originate
from different genes or gene families (α1–α6, β1–β3, γ1–γ3, δ, ε, θ, π, or ρ1–3). In the mouse …

Cryo-EM structure of the benzodiazepine-sensitive α1β1γ2S tri-heteromeric GABAA receptor in complex with GABA

S Phulera, H Zhu, J Yu, DP Claxton, N Yoder… - Elife, 2018 - elifesciences.org
Fast inhibitory neurotransmission in the mammalian nervous system is largely mediated by
GABAA receptors, chloride-selective members of the superfamily of pentameric Cys-loop …

Allosteric modulation of GABAA receptors via multiple drug-binding sites

W Sieghart - Advances in pharmacology, 2015 - Elsevier
GABA A receptors are ligand-gated ion channels composed of five subunits that can be
opened by GABA and be modulated by multiple pharmacologically and clinically important …

Long-term diazepam treatment enhances microglial spine engulfment and impairs cognitive performance via the mitochondrial 18 kDa translocator protein (TSPO)

Y Shi, M Cui, K Ochs, M Brendel, FL Strübing… - Nature …, 2022 - nature.com
Benzodiazepines are widely administered drugs to treat anxiety and insomnia. In addition to
tolerance development and abuse liability, their chronic use may cause cognitive …