Propofol is an allosteric agonist with multiple binding sites on concatemeric ternary GABAA receptors

DJ Shin, AL Germann, AD Johnson, SA Forman… - Molecular …, 2018 - ASPET
… Molecular structures of the putative propofol binding sites at various … To define the number
of functional propofol-binding sites … at locations outside of the putative propofol-binding sites

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
… A, the α 1 β 2 γ 2 GABA A receptor is composed of two α, two β and a γ subunit(s). Two
GABA binding sites are located at the two β+/α− subunit interfaces. The scheme shows the …

Binding site location on GABAA receptors determines whether mixtures of intravenous general anaesthetics interact synergistically or additively in vivo

DE Kent, PY Savechenkov, KS Bruzik… - British Journal of …, 2019 - Wiley Online Library
… We chose propofol to test the hypothesis that agents with weak … sites are likely to exist
in all GABA A receptors. An additional complexity is that some receptors may have no well-defined

Analysis of GABAA receptor activation by combinations of agonists acting at the same or distinct binding sites

DJ Shin, AL Germann, DF Covey, JH Steinbach… - Molecular …, 2019 - ASPET
… infer that the actions of GABA and propofol can be described … act on the GABA A receptor
through distinct binding sites. Both … in which GABA (N GABA = 2) and propofol (N propofol = 6) …

Comparison of αβδ and αβγ GABAA receptors: Allosteric modulation and identification of subunit arrangement by site-selective general anesthetics

HJ Feng, SA Forman - Pharmacological research, 2018 - Elsevier
GABA binding sites on typical synaptic αβγ GABA A receptorsidentifying GABA A receptor
sites for four potent anesthetics. … Akabas to test propofol interactions in GABA A receptors [146] …

Identifying drugs that bind selectively to intersubunit general anesthetic sites in the α1β3γ2 GABAAR transmembrane domain

SS Jayakar, X Zhou, DC Chiara, C Jarava-Barrera… - Molecular …, 2019 - ASPET
… at postsynaptic sites, GABA binding sites are located in the … binding of GABA A R PAMs to
the intersubunit binding sites in the … of a panel of propofol derivatives and structurally unrelated …

Mapping general anesthetic sites in heteromeric γ-aminobutyric acid type A receptors reveals a potential for targeting receptor subtypes

SA Forman, KW Miller - Anesthesia & Analgesia, 2016 - journals.lww.com
… Our goal of identifying anesthetic-binding sites in GABA A Rs has required a number of …
-, barbiturate-, and propofol-binding sites on GABA A Rs are located in homologous pockets …

[HTML][HTML] Identification of binding sites contributing to volatile anesthetic effects on GABA type A receptors

KA Woll, X Zhou, NV Bhanu, BA Garcia… - The FASEB …, 2018 - ncbi.nlm.nih.gov
… focused largely on identifying binding sites for iv anesthetics, such as propofol, etomidate, …
Our study also demonstrated a shared ISO and SEVO binding site that is located within the β…

GABAA receptor: Positive and negative allosteric modulators

RW Olsen - Neuropharmacology, 2018 - Elsevier
… The GABA binding sites were located in the ECD of the receptor protein by affinity labeling …
a channel blocker, then we have defined how picrotoxin acts as a NAM to GABA and we don't …

The role of GABA receptor agonists in anesthesia and sedation

J Brohan, BG Goudra - CNS drugs, 2017 - Springer
… Neurotransmitter binding sites are located at two or more … -defined GABA B receptors (GABABRs)
are transmembrane … the liberated propofol, subsequently potentiating GABA-inhibitory …