Direct structural insights into GABAA receptor pharmacology

JJ Kim, RE Hibbs - Trends in biochemical sciences, 2021 - cell.com
GABA A receptors are pentameric ligand-gated ion channels that mediate most fast
neuronal inhibition in the brain. In addition to their important physiological roles, they are …

Molecular structure and function of the glycine receptor chloride channel

JW Lynch - Physiological reviews, 2004 - journals.physiology.org
The glycine receptor chloride channel (GlyR) is a member of the nicotinic acetylcholine
receptor family of ligand-gated ion channels. Functional receptors of this family comprise five …

[HTML][HTML] Shared structural mechanisms of general anaesthetics and benzodiazepines

JJ Kim, A Gharpure, J Teng, Y Zhuang, RJ Howard… - Nature, 2020 - nature.com
Most general anaesthetics and classical benzodiazepine drugs act through positive
modulation of γ-aminobutyric acid type A (GABAA) receptors to dampen neuronal activity in …

Studies on the mechanism of general anesthesia

MA Pavel, EN Petersen, H Wang… - Proceedings of the …, 2020 - National Acad Sciences
Inhaled anesthetics are a chemically diverse collection of hydrophobic molecules that
robustly activate TWIK-related K+ channels (TREK-1) and reversibly induce loss of …

[HTML][HTML] Molecular and neuronal substrates for general anaesthetics

U Rudolph, B Antkowiak - Nature Reviews Neuroscience, 2004 - nature.com
Although general anaesthesia has been of tremendous importance for the development of
surgery, the underlying mechanisms by which this state is achieved are only just beginning …

Clinical and molecular pharmacology of etomidate

SA Forman, DS Warner - The Journal of the American Society of …, 2011 - pubs.asahq.org
This review focuses on the unique clinical and molecular pharmacologic features of
etomidate. Among general anesthesia induction drugs, etomidate is the only imidazole, and …

[HTML][HTML] The anesthetic mechanism of urethane: the effects on neurotransmitter-gated ion channels

K Hara, RA Harris - Anesthesia & Analgesia, 2002 - journals.lww.com
Urethane is widely used as an anesthetic for animal studies because of its minimal effects
on cardiovascular and respiratory systems and maintenance of spinal reflexes. Despite its …

[HTML][HTML] The sedative component of anesthesia is mediated by GABAA receptors in an endogenous sleep pathway

LE Nelson, TZ Guo, J Lu, CB Saper, NP Franks… - Nature …, 2002 - nature.com
We investigated the role of regionally discrete GABA (γ-aminobutyric acid) receptors in the
sedative response to pharmacological agents that act on GABAA receptors (muscimol …

General anesthetic actions in vivo strongly attenuated by a point mutation in the GABAA receptor β3 subunit

R Jurd, M Arrasa, S Lambert, B Drexler… - The FASEB …, 2003 - Wiley Online Library
General anesthetics are widely used in clinical practice. On the molecular level, these
compounds have been shown to modulate the activity of various neuronal ion channels …

Emerging molecular mechanisms of general anesthetic action

HC Hemmings, MH Akabas, PA Goldstein… - Trends in …, 2005 - cell.com
General anesthetics are essential to modern medicine, and yet a detailed understanding of
their mechanisms of action is lacking. General anesthetics were once believed to be 'drugs …