Opposing effects of the anesthetic propofol at pentameric ligand-gated ion channels mediated by a common site

T Lynagh, B Laube - Journal of Neuroscience, 2014 - Soc Neuroscience
Propofol is an intravenous general anesthetic that alters neuronal excitability by modulating
agonist responses of pentameric ligand-gated ion channels (pLGICs). Evidence suggests …

Genistein exerts potent antitumour effects alongside anaesthetic, propofol, by suppressing cell proliferation and nuclear factor-κB-mediated signalling and through …

Y Zheng, H Liu, Y Liang - Journal of Pharmacy and …, 2017 - academic.oup.com
Objective This study was implemented to evaluate the effect of genistein and propofol on
intracranial tumour model. Methods Male Fischer 344 rats were subjected to intracranial …

p-Trifluoromethyldiazirinyl-etomidate: A Potent Photoreactive General Anesthetic Derivative of Etomidate That Is Selective for Ligand-Gated Cationic Ion Channels

SS Husain, D Stewart, R Desai… - Journal of medicinal …, 2010 - ACS Publications
We synthesized the R-and S-enantiomers of ethyl 1-(1-(4-(3-((trifluoromethyl)-3 H-diazirin-3-
yl) phenyl) ethyl)-1 H-imidazole-5-carboxylate (trifluoromethyldiazirinyl-etomidate), or TFD …

Filling the Gap in Understanding the Mechanism of GABAAR and Propofol Using Computational Approaches

X Yuan, D Zhang, S Mao, Q Wang - Journal of Chemical …, 2021 - ACS Publications
γ-Aminobutyric acid type-A receptors (GABAARs) play a critical role in neural transmission
by mediating the inhibitory neural firing and are the target of many psychiatric drugs. Among …

Intravenous anesthetic propofol suppresses prostaglandin E2 production in murine dendritic cells

T Inada, K Kubo, H Ueshima… - Journal of …, 2011 - Taylor & Francis
Propofol is an intravenous anesthetic that is widely used for anesthesia and sedation.
Dendritic cells (DC) are one of the crucial immune cells that bridge innate and adaptive …

[HTML][HTML] γ-aminobutyric acid (GABA) and pentobarbital induce different conformational rearrangements in the GABAA receptor α1 and β2 pre-M1 regions

J Mercado, C Czajkowski - Journal of Biological Chemistry, 2008 - ASBMB
γ-Aminobutyric acid (GABA) binding to GABA A receptors (GABA A Rs) triggers
conformational movements in the α 1 and β 2 pre-M1 regions that are associated with …

Evidence for peripherally antinociceptive action of propofol in rats: behavioral and spinal neuronal responses to subcutaneous bee venom

YY Sun, KC Li, J Chen - Brain research, 2005 - Elsevier
In the present study, behavioral and in vivo electrophysiological methods were used to
examine the peripheral effects of propofol on tonic ongoing pain-related responses …

Substituted Cysteine Modification and Protection with n-Alkyl-MTS Reagents Quantifies Steric Changes Induced by a Mutation in Anesthetic Binding Sites on GABA …

K Bhave, SA Forman - Molecular Pharmacology, 2023 - ASPET
Multiple approaches, including cryogenic electron microscopy (cryo-EM), indicate that the
anesthetics etomidate and propofol modulate α 1 β 2/3 γ 2 GABAA receptors by binding in …

Investigation of 2, 6-diisopropylphenol (propofol)-evoked Ca2+ movement and cell death in human glioblastoma cells

WZ Liang, CR Jan, CH Lu - Toxicology in Vitro, 2012 - Elsevier
This study examined whether propofol altered [Ca2+] i and caused cell death in DBTRG-
05MG cells. Propofol at 400–1000μM increased [Ca2+] i in a concentration-dependent …

[HTML][HTML] Gating-induced conformational rearrangement of the γ-aminobutyric acid type A receptor β-α subunit interface in the membrane-spanning domain

M Bali, MH Akabas - Journal of Biological Chemistry, 2012 - ASBMB
GABA A receptors mediate fast inhibitory synaptic transmission. The transmembrane ion
channel is lined by a ring of five α helices, M2 segments, one from each subunit. An outer …