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 …

Heterogeneity of GABAA receptors: revived interest in the development of subtype-selective drugs

W Sieghart, M Ernst - Current Medicinal Chemistry-Central …, 2005 - ingentaconnect.com
Gamma-aminobutyric acid (GABA) is the most important inhibitory transmitter in the central
nervous system. Most of the actions of GABA are mediated by GABAA receptors. These are …

GABA receptors: pharmacological potential and pitfalls

M Jazvinscak Jembrek, J Vlainic - Current pharmaceutical …, 2015 - ingentaconnect.com
Gamma-amino butyric acid (GABA), the major inhibitory neurotransmitter in the mammalian
central nervous system, plays a key role in the regulation of neuronal transmission …

GABAA receptor partial agonists and antagonists: structure, binding mode, and pharmacology

J Krall, T Balle, N Krogsgaard-Larsen… - Advances in …, 2015 - Elsevier
A high degree of structural heterogeneity of the GABA A receptors (GABA A Rs) has been
revealed and is reflected in multiple receptor subtypes. The subunit composition of GABA …

Unraveling the function of GABAA receptor subtypes

W Sieghart - Trends in pharmacological sciences, 2000 - cell.com
GABA A receptors are Cl− channels that can be opened by GABA and are the major
inhibitory neurotransmitter receptors in the CNS. A variety of pharmacologically important …

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 …

Interaction of allosteric ligands with GABAA receptors containing one, two, or three different subunits

J Zezula, A Slany, W Sieghart - European journal of pharmacology, 1996 - Elsevier
The presence of allosteric binding sites on recombinant GABAA receptors formed after
transfection of human embryonic kidney (HEK) 293 cells with α1-, β3-, γ2-subunits, or with …

GABAA receptors and the diversity in their structure and pharmacology

HC Chua, M Chebib - Advances in pharmacology, 2017 - Elsevier
Abstract GABA A receptors (GABA A Rs) are a class of ligand-gated ion channels with high
physiological and therapeutic significance. In the brain, these pentameric receptors occur …

Allosteric ligands and their binding sites define γ-aminobutyric acid (GABA) type A receptor subtypes

RW Olsen - Advances in Pharmacology, 2015 - Elsevier
Abstract GABA A receptors (GABA A Rs) mediate rapid inhibitory transmission in the brain.
GABA A Rs are ligand-gated chloride ion channel proteins and exist in about a dozen or …

[HTML][HTML] Four amino acids in the α subunits determine the γ-aminobutyric acid sensitivities of GABAA receptor subtypes

I Böhme, H Rabe, H Luddens - Journal of Biological Chemistry, 2004 - ASBMB
GABA A receptors, mediators of fast inhibitory neurotransmission, are heteropentameric
assemblies from a large array of subunits. Differences in the sensitivity of receptor subtypes …