A propofol binding site on mammalian GABAA receptors identified by photolabeling
GMS Yip, ZW Chen, CJ Edge, EH Smith… - Nature chemical …, 2013 - nature.com
Propofol is the most important intravenous general anesthetic in current clinical use. It acts
by potentiating GABAA (γ-aminobutyric acid type A) receptors, but where it binds to this …
by potentiating GABAA (γ-aminobutyric acid type A) receptors, but where it binds to this …
Defining the propofol binding site location on the GABAA receptor
M Bali, MH Akabas - Molecular pharmacology, 2004 - ASPET
The GABAA receptor is a target of many general anesthetics. The low affinity of general
anesthetics has complicated the search for the location of anesthetic binding sites. Attention …
anesthetics has complicated the search for the location of anesthetic binding sites. Attention …
Multiple Propofol-binding Sites in a γ-Aminobutyric Acid Type A Receptor (GABAAR) Identified Using a Photoreactive Propofol Analog*♦
SS Jayakar, X Zhou, DC Chiara, Z Dostalova… - Journal of Biological …, 2014 - ASBMB
Propofol acts as a positive allosteric modulator of γ-aminobutyric acid type A receptors
(GABA A Rs), an interaction necessary for its anesthetic potency in vivo as a general …
(GABA A Rs), an interaction necessary for its anesthetic potency in vivo as a general …
Methionine 286 in transmembrane domain 3 of the GABAA receptor β subunit controls a binding cavity for propofol and other alkylphenol general anesthetics
MD Krasowski, K Nishikawa, N Nikolaeva, A Lin… - …, 2001 - Elsevier
γ-Aminobutyric acid type A (GABAA) receptors are an important target for general
anesthetics in the central nervous system. Site-directed mutagenesis techniques have …
anesthetics in the central nervous system. Site-directed mutagenesis techniques have …
An allosteric coagonist model for propofol effects on α1β2γ2L γ-aminobutyric acid type A receptors
D Ruesch, E Neumann, H Wulf… - The Journal of the …, 2012 - pubs.asahq.org
Background Propofol produces its major actions via γ-aminobutyric acid type A (GABA (A))
receptors. At low concentrations, propofol enhances agonist-stimulated GABA (A) receptor …
receptors. At low concentrations, propofol enhances agonist-stimulated GABA (A) receptor …
Specificity of Intersubunit General Anesthetic-binding Sites in the Transmembrane Domain of the Human α1β3γ2 γ-Aminobutyric Acid Type A (GABAA) Receptor*♦
DC Chiara, SS Jayakar, X Zhou, X Zhang… - Journal of Biological …, 2013 - ASBMB
GABA type A receptors (GABA AR), the brain's major inhibitory neurotransmitter receptors,
are the targets for many general anesthetics, including volatile anesthetics, etomidate …
are the targets for many general anesthetics, including volatile anesthetics, etomidate …
[PDF][PDF] Actions of the general anesthetic propofol on recombinant human GABAA receptors: influence of receptor subunits.
E Sanna, MP Mascia, RL Klein, PJ Whiting… - … of Pharmacology and …, 1995 - Citeseer
ABSTRACT The intravenous general anesthetic 2, 6-diisopropylphenol (propofol)
potentiates GABAA receptor function, but the precise mechanisms and specificity of this …
potentiates GABAA receptor function, but the precise mechanisms and specificity of this …
Functional sites involved in modulation of the GABAA receptor channel by the intravenous anesthetics propofol, etomidate and pentobarbital
MC Maldifassi, R Baur, E Sigel - Neuropharmacology, 2016 - Elsevier
GABA A receptors are the major inhibitory neurotransmitter receptors in the brain and are
the target for many clinically important drugs. Among the many modulatory compounds are …
the target for many clinically important drugs. Among the many modulatory compounds are …
Propofol Analogues. Synthesis, Relationships between Structure and Affinity at GABAA Receptor in Rat Brain, and Differential Electrophysiological Profile at Recombinant …
G Trapani, A Latrofa, M Franco… - Journal of medicinal …, 1998 - ACS Publications
A number of propofol (2, 6-diisopropylphenol) congeners and derivatives were synthesized
and their in vitro capability to affect GABAA receptors determined by the inhibition of the …
and their in vitro capability to affect GABAA receptors determined by the inhibition of the …
Molecular targets underlying general anaesthesia
NP Franks - British journal of pharmacology, 2006 - Wiley Online Library
The discovery of general anaesthesia, over 150 years ago, revolutionised medicine. The
ability to render a patient unconscious and insensible to pain made modern surgery …
ability to render a patient unconscious and insensible to pain made modern surgery …