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 …

The benzodiazepine binding sites of GABAA receptors

E Sigel, M Ernst - Trends in pharmacological sciences, 2018 - cell.com
Everyday activity is based on a subtle equilibrium of excitatory and inhibitory neuronal
systems. The most prominent players in neuronal inhibition are synaptic and extrasynaptic …

Structure of a human synaptic GABAA receptor

S Zhu, CM Noviello, J Teng, RM Walsh Jr, JJ Kim… - Nature, 2018 - nature.com
Fast inhibitory neurotransmission in the brain is principally mediated by the neurotransmitter
GABA (γ-aminobutyric acid) and its synaptic target, the type A GABA receptor (GABAA …

[图书][B] As Bases Farmacológicas da Terapêutica de Goodman e Gilman-13

LL Brunton, R Hilal-Dandan, BC Knollmann - 2018 - books.google.com
A bíblia azul da farmacologia–assim tem sido mundialmente chamado este clássico
acadêmico desde o lançamento de sua 1ª edição, em 1941. A nova edição de Goodman & …

The direct actions of cannabidiol and 2-arachidonoyl glycerol at GABAA receptors

T Bakas, PS Van Nieuwenhuijzen, SO Devenish… - Pharmacological …, 2017 - Elsevier
Cannabidiol (CBD) is a major non-intoxicating component of cannabis and possesses anti-
epileptic, anxiolytic and anti-hyperalgesic properties. The mechanism of action of CBD in …

International Union of Basic and Clinical Pharmacology. CVI: GABAA receptor subtype-and function-selective ligands: key issues in translation to humans

W Sieghart, MM Savić - Pharmacological reviews, 2018 - ASPET
GABAA receptors are the major inhibitory transmitter receptors in the brain. They are ligand-
gated chloride channels and the site of action of benzodiazepines, barbiturates, neuroactive …

GABAergic dysfunction in excitatory and inhibitory (E/I) imbalance drives the pathogenesis of Alzheimer's disease

D Bi, L Wen, Z Wu, Y Shen - Alzheimer's & Dementia, 2020 - Wiley Online Library
Objective To propose a new hypothesis that GABAergic dysfunction in excitatory and
inhibitory (E/I) imbalance drives the pathogenesis of Alzheimer's disease (AD). Background …

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 …

Allopregnanolone: An overview on its synthesis and effects

S Diviccaro, L Cioffi, E Falvo, S Giatti… - Journal of …, 2022 - Wiley Online Library
Abstract Allopregnanolone, a 3α, 5α‐progesterone metabolite, acts as a potent allosteric
modulator of the γ‐aminobutyric acid type A receptor. In the present review, the synthesis of …

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 …