Neurosteroids: endogenous regulators of the GABAA receptor

D Belelli, JJ Lambert - Nature Reviews Neuroscience, 2005 - nature.com
GABAA (γ-aminobutyric acid type A) receptors mediate most of the'fast'synaptic inhibition in
the mammalian brain and are targeted by many clinically important drugs. Certain naturally …

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 …

Allosteric binding sites on cell-surface receptors: novel targets for drug discovery

A Christopoulos - Nature reviews Drug discovery, 2002 - nature.com
Cell-surface receptors are the targets for more than 60% of current drugs. Traditionally,
optimizing the interaction of lead molecules with the binding site for the endogenous agonist …

Thymol, a constituent of thyme essential oil, is a positive allosteric modulator of human GABAA receptors and a homo‐oligomeric GABA receptor from Drosophila …

CM Priestley, EM Williamson… - British journal of …, 2003 - Wiley Online Library
The GABA‐modulating and GABA‐mimetic activities of the monoterpenoid thymol were
explored on human GABAA and Drosophila melanogaster homomeric RDLac GABA …

Iron overload contributes to general anaesthesia-induced neurotoxicity and cognitive deficits

J Wu, JJ Yang, Y Cao, H Li, H Zhao, S Yang… - Journal of …, 2020 - Springer
Background Increasing evidence suggests that multiple or long-time exposure to general
anaesthesia (GA) could be detrimental to cognitive development in young subjects and …

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 …

Neurosteroid modulation of GABAA receptors

JJ Lambert, D Belelli, DR Peden, AW Vardy… - Progress in …, 2003 - Elsevier
Certain metabolites of progesterone and deoxycorticosterone are established as potent and
selective positive allosteric modulators of the γ-aminobutyric acid type A (GABAA) receptor …

Extrasynaptic GABAA receptors of thalamocortical neurons: a molecular target for hypnotics

D Belelli, DR Peden, TW Rosahl, KA Wafford… - Journal of …, 2005 - jneurosci.org
Among hypnotic agents that enhance GABAA receptor function, etomidate is unusual
because it is selective for β2/β3 compared with β1 subunit-containing GABAA receptors …

The TREK K2P channels and their role in general anaesthesia and neuroprotection

NP Franks, E Honoré - Trends in Pharmacological Sciences, 2004 - cell.com
Two-pore-domain K+(K 2P) channels are a diverse and highly regulated superfamily of
channels that are thought to provide baseline regulation of membrane excitability. Of these …

Anesthetics and ion channels: molecular models and sites of action

T Yamakura, E Bertaccini, JR Trudell… - Annual review of …, 2001 - annualreviews.org
The mechanisms of general anesthesia in the central nervous system are finally yielding to
molecular examination. As a result of research during the past several decades, a group of …