GABAA receptor: Positive and negative allosteric modulators

RW Olsen - Neuropharmacology, 2018 - Elsevier
Abstract gamma-Aminobutyric acid (GABA)-mediated inhibitory neurotransmission and the
gene products involved were discovered during the mid-twentieth century. Historically …

General anaesthesia: from molecular targets to neuronal pathways of sleep and arousal

NP Franks - Nature Reviews Neuroscience, 2008 - nature.com
The mechanisms through which general anaesthetics, an extremely diverse group of drugs,
cause reversible loss of consciousness have been a long-standing mystery. Gradually, a …

GABAA receptors: subtypes provide diversity of function and pharmacology

RW Olsen, W Sieghart - Neuropharmacology, 2009 - Elsevier
This mini-review attempts to update experimental evidence on the existence of GABAA
receptor pharmacological subtypes and to produce a list of those native receptors that exist …

Diazirine based photoaffinity labeling

L Dubinsky, BP Krom, MM Meijler - Bioorganic & medicinal chemistry, 2012 - Elsevier
Diazirines are among the smallest photoreactive groups that form a reactive carbene upon
light irradiation. This feature has been widely utilized in photoaffinity labeling to study ligand …

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 …

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 …

Allosteric modulation of GABAA receptors via multiple drug-binding sites

W Sieghart - Advances in pharmacology, 2015 - Elsevier
GABA A receptors are ligand-gated ion channels composed of five subunits that can be
opened by GABA and be modulated by multiple pharmacologically and clinically important …

Binding, activation and modulation of Cys-loop receptors

PS Miller, TG Smart - Trends in pharmacological sciences, 2010 - cell.com
It is over forty years since the major neurotransmitters and their protein receptors were
identified, and over twenty years since determination of the first amino-acid sequences 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 …

Structure, pharmacology, and function of GABAA receptor subtypes

W Sieghart - Advances in pharmacology, 2006 - Elsevier
Publisher Summary This chapter describes the structure, pharmacology, and function of γ‐
aminobutyric acid type A (GABA A) receptor subtypes. GABA A receptors are the most …