GABA (A) receptor-targeted drug development-New perspectives in perioperative anesthesia

B Antkowiak, G Rammes - Expert opinion on drug discovery, 2019 - Taylor & Francis
Introduction: Perioperative anesthesia delivers pre-, intra-, and postoperative care to meet
the needs of patients undergoing diagnostic and surgical procedures. Major challenges are …

Time to wake up! The ongoing search for general anesthetic reversal agents

DM Cylinder, AAJ van Zundert, K Solt… - …, 2024 - ingentaconnect.com
How general anesthetics work remains a topic of ongoing study. A parallel field of research
has sought to identify methods to reverse general anesthesia. Reversal agents could …

Selective actions of benzodiazepines at the transmembrane anaesthetic binding sites of the GABAA receptor: In vitro and in vivo studies

M McGrath, H Hoyt, A Pence… - British journal of …, 2021 - Wiley Online Library
Background and Purpose In addition to binding to the classical high‐affinity extracellular
benzodiazepine binding site of the GABAA receptor, some benzodiazepines occupy …

General anaesthetics as 'awakening agents'? Re‐appraising the evidence for suggested 'pressure reversal'of anaesthesia

BM George, JJ Pandit - Clinical and Experimental …, 2021 - Wiley Online Library
Increasing ambient pressure has been suggested to reverse general anaesthesia and
provides support for the 'lipid theory'. Anaesthetic dissolution into cell membranes is said to …

Competitive interactions between halothane and isoflurane at the carotid body and TASK channels

JJ Pandit, N Huskens, PB O'Donohoe… - …, 2020 - ingentaconnect.com
Background: The degree to which different volatile anesthetics depress carotid body hypoxic
response relates to their ability to activate TASK potassium channels. Most commonly …

Competitive antagonism of etomidate action by diazepam: in vitro GABAA receptor and in vivo zebrafish studies

M McGrath, H Hoyt, A Pence, SS Jayakar… - …, 2020 - pmc.ncbi.nlm.nih.gov
Background: Recent cryo-electron microscopic imaging studies have shown that in addition
to binding to the classical extracellular benzodiazepine binding site of the α1β3γ2L γ …

Etomidate and etomidate analog binding and positive modulation of γ-aminobutyric acid type A receptors: evidence for a state-dependent cutoff effect

M McGrath, Z Yu, SS Jayakar, C Ma, M Tolia… - …, 2018 - pmc.ncbi.nlm.nih.gov
Background: Naphthalene-etomidate, an etomidate analog containing a bulky phenyl ring
substituent group, possesses very low γ-aminobutyric acid type A (GABAA) receptor efficacy …

[HTML][HTML] Antagonism of Propofol Anesthesia by Alkyl-fluorobenzene Derivatives

DM Plasencia, LH Rodgers, AR Knighton… - Research …, 2024 - ncbi.nlm.nih.gov
Despite their frequent use across many clinical settings, general anesthetics are
medications with lethal side effects and no reversal agents. A fluorinated analogue of …

[PDF][PDF] 基于膜电位检测原理的γ-氨基丁酸A 型受体药物高通量筛选模型

张毅, 石童, 张瑞华, 陈学军, 靳倩… - 中国药理学与毒 …, 2022 - cjpt.magtechjournal.com
目的利用膜电位检测原理, 构建一种靶向γ-氨基丁酸A 型受体(GABAAR) 的药物高通量筛选模型.
方法采用α1β2γ2L-GABAAR-CHO 细胞株构建GABAAR 药物高通量筛选方法; …

The effects of a competitive antagonist on GABA-evoked currents in the presence of sedative-hypnotic agents

M McGrath, M Tolia, DE Raines - Pharmacological Reports, 2020 - Springer
Background Many sedative-hypnotic agents are thought to act by positively modulating γ-
aminobutyric acid type A (GABA A) receptors. However, for many agents, the location (s) of …