[HTML][HTML] Cysteine substitutions define etomidate binding and gating linkages in the α-M1 domain of γ-aminobutyric acid type A (GABAA) receptors

DS Stewart, M Hotta, G Li, R Desai, DC Chiara… - Journal of Biological …, 2013 - ASBMB
Etomidate is a potent general anesthetic that acts as an allosteric co-agonist at GABA A
receptors. Photoreactive etomidate derivatives labeled αMet-236 in transmembrane domain …

Disrupted Cl homeostasis contributes to reductions in the inhibitory efficacy of diazepam during hyperexcited states

TZ Deeb, Y Nakamura, GD Frost… - European Journal of …, 2013 - Wiley Online Library
The K+‐Cl− cotransporter type 2 is the major Cl− extrusion mechanism in most adult
neurons. This process in turn leads to Cl− influx upon activation of γ‐aminobutyric acid type …

In Search of GABAA Receptor's Neurosteroid Binding Sites: Miniperspective

LD Alvarez, A Pecci, DA Estrin - Journal of Medicinal Chemistry, 2018 - ACS Publications
Neurosteroids (NS) are the main modulators of γ-aminobutyric acid type A receptors
(GABAARs), which are the ligand-gated channels target of the major inhibitory …

Anaesthetic binding sites for etomidate and propofol on a GABAA receptor model

V Campagna-Slater, DF Weaver - Neuroscience letters, 2007 - Elsevier
Investigating the molecular basis of general anaesthetic activity at the GABAA ligand-gated
ion channel is challenging due to the wide structural diversity among known general …

[HTML][HTML] Changes in effective connectivity by propofol sedation

F Gomez, C Phillips, A Soddu, M Boly, P Boveroux… - PLoS …, 2013 - journals.plos.org
Mechanisms of propofol-induced loss of consciousness remain poorly understood. Recent
fMRI studies have shown decreases in functional connectivity during unconsciousness …

Experimental determination of the vertical alignment between the second and third transmembrane segments of muscle nicotinic acetylcholine receptors

N Mnatsakanyan, M Jansen - Journal of neurochemistry, 2013 - Wiley Online Library
Nicotinic acetylcholine receptors (nAChR) are members of the Cys‐loop ligand‐gated ion
channel superfamily. Muscle nAChR are heteropentamers that assemble from two α, and …

Explaining general anesthesia: A two‐step hypothesis linking sleep circuits and the synaptic release machinery

B van Swinderen, B Kottler - Bioessays, 2014 - Wiley Online Library
Several general anesthetics produce their sedative effect by activating endogenous sleep
pathways. We propose that general anesthesia is a two‐step process targeting sleep circuits …

State-dependent cross-linking of the M2 and M3 segments: functional basis for the alignment of GABAA and acetylcholine receptor M3 segments

M Jansen, MH Akabas - Journal of Neuroscience, 2006 - Soc Neuroscience
Construction of a GABAA receptor homology model based on the acetylcholine (ACh)
receptor structure is complicated by the low sequence similarity between GABAA and ACh …

[HTML][HTML] Membrane nanodomains homeostasis during propofol anesthesia as function of dosage and temperature

W Jin, M Zucker, A Pralle - Biochimica et Biophysica Acta (BBA) …, 2021 - Elsevier
Some anesthetics bind and potentiate γ-aminobutyric-acid-type receptors, but no universal
mechanism for general anesthesia is known. Furthermore, often encountered complications …

[HTML][HTML] Phenols and GABAA receptors: from structure and molecular mechanisms action to neuropsychiatric sequelae

SA Menzikov, DM Zaichenko, AA Moskovtsev… - Frontiers in …, 2024 - frontiersin.org
γ-Aminobutyric acid type A receptors (GABAARs) are members of the pentameric ligand-
gated ion channel (pLGIC) family, which are widespread throughout the invertebrate and …