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, EH Ohlstein - Pharmacological reviews, 2018 - Elsevier
GABA A 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 …

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 …

Differential assembly diversifies GABAA receptor structures and signalling

A Sente, R Desai, K Naydenova, T Malinauskas… - Nature, 2022 - nature.com
Type A γ-aminobutyric acid receptors (GABAARs) are pentameric ligand-gated chloride
channels that mediate fast inhibitory signalling in neural circuits, and can be modulated by …

[HTML][HTML] Extrasynaptic δ-subunit containing GABAA receptors

A Arslan - Journal of integrative neuroscience, 2021 - imrpress.com
γ-Aminobutyric acid type A receptors (GABAARs) are GABA gated heteropentameric
chloride channels responsible for the adult brain's primary inhibition. In specific brain cells …

Delta-containing GABAA receptors in pain management: Promising targets for novel analgesics

Y Luo, AS Kusay, T Jiang, M Chebib, T Balle - Neuropharmacology, 2021 - Elsevier
Communication between nerve cells depends on the balance between excitatory and
inhibitory circuits. GABA, the major inhibitory neurotransmitter, regulates this balance and …

Comparison of αβδ and αβγ GABAA receptors: Allosteric modulation and identification of subunit arrangement by site-selective general anesthetics

HJ Feng, SA Forman - Pharmacological research, 2018 - Elsevier
GABA A receptors play a dominant role in mediating inhibition in the mature mammalian
brain, and defects of GABAergic neurotransmission contribute to the pathogenesis of a …

Identification of a New Pyrazolo[1,5-a]quinazoline Ligand Highly Affine to γ-Aminobutyric Type A (GABAA) Receptor Subtype with Anxiolytic-Like and …

G Guerrini, G Ciciani, L Crocetti, S Daniele… - Journal of medicinal …, 2017 - ACS Publications
Compounds that can act on GABAA receptor subtype in a selective manner, without the side
effects of classical benzodiazepine ligands, represent promising therapeutic tools in …

General anesthetic binding sites in human α4β3δ γ-aminobutyric acid type A receptors (GABAARs)

DC Chiara, Y Jounaidi, X Zhou… - Journal of Biological …, 2016 - ASBMB
Extrasynaptic γ-aminobutyric acid type A receptors (GABA A Rs), which contribute
generalized inhibitory tone to the mammalian brain, are major targets for general …

GABA beyond the synapse: defining the subtype‐specific pharmacodynamics of non‐synaptic GABAA receptors

AH Lagrange, NN Hu… - The Journal of physiology, 2018 - Wiley Online Library
Key points Physiologically relevant combinations of recombinant GABAA receptor (GABAR)
subunits were expressed in HEK293 cells. Using whole‐cell voltage clamp and rapid drug …

Virally-induced expression of GABAA receptor δ subunits following their pathological loss reveals their role in regulating GABAA receptor assembly

Y Sun, Z Peng, X Wei, N Zhang, CS Huang… - Progress in …, 2022 - Elsevier
Decreased expression of the δ subunit of the GABA A receptor (GABA AR) has been found
in the dentate gyrus in several animal models of epilepsy and other disorders with increased …