GABA Receptors and the Pharmacology of Sleep.
Sign Up to like & getrecommendations! Published in 2017 at "Handbook of experimental pharmacology"
DOI: 10.1007/164_2017_56
Abstract: Current GABAergic sleep-promoting medications were developed pragmatically, without making use of the immense diversity of GABAA receptors. Pharmacogenetic experiments are leading to an understanding of the circuit mechanisms in the hypothalamus by which zolpidem and… read more here.
Keywords: gaba receptors; pharmacology; gabaa receptors; receptors pharmacology ... See more keywords
Electrophysiology of ionotropic GABA receptors
Sign Up to like & getrecommendations! Published in 2021 at "Cellular and Molecular Life Sciences"
DOI: 10.1007/s00018-021-03846-2
Abstract: GABAA receptors are ligand-gated chloride channels and ionotropic receptors of GABA, the main inhibitory neurotransmitter in vertebrates. In this review, we discuss the major and diverse roles GABAA receptors play in the regulation of neuronal… read more here.
Keywords: electrophysiology ionotropic; gaba receptors; ionotropic gaba; gabaa receptors ... See more keywords
The role of hippocampal GABAA receptors on anxiolytic effects of Echium amoenum extract in a mice model of restraint stress
Sign Up to like & getrecommendations! Published in 2020 at "Molecular Biology Reports"
DOI: 10.1007/s11033-020-05699-7
Abstract: Echium amoenum (EA), a popular medicinal plant in Persian medicine, has anxiolytic, antioxidant, sedative, and anti-inflammatory effects. This study examined whether GABA-ergic signaling is involved in the anxiolytic effects of EA in mice. Sixty BALB/c… read more here.
Keywords: anxiolytic effects; gabaa receptors; restraint stress; mice ... See more keywords
An Essential Role for the Tetraspanin LHFPL4 in the Cell-Type-Specific Targeting and Clustering of Synaptic GABAA Receptors
Sign Up to like & getrecommendations! Published in 2017 at "Cell Reports"
DOI: 10.1016/j.celrep.2017.09.025
Abstract: Summary Inhibitory synaptic transmission requires the targeting and stabilization of GABAA receptors (GABAARs) at synapses. The mechanisms responsible remain poorly understood, and roles for transmembrane accessory proteins have not been established. Using molecular, imaging, and… read more here.
Keywords: tetraspanin lhfpl4; type specific; gabaa receptors; cell type ... See more keywords
Sparsification of AP firing in adult-born hippocampal granule cells via voltage-dependent α5-GABAA receptors.
Sign Up to like & getrecommendations! Published in 2021 at "Cell reports"
DOI: 10.1016/j.celrep.2021.109768
Abstract: GABA can depolarize immature neurons close to the action potential (AP) threshold in development and adult neurogenesis. Nevertheless, GABAergic synapses effectively inhibit AP firing in newborn granule cells of the adult hippocampus as early as… read more here.
Keywords: adult; hippocampal granule; voltage dependent; gabaa receptors ... See more keywords
Functional Characterization of Native, High-Affinity GABAA Receptors in Human Pancreatic β Cells
Sign Up to like & getrecommendations! Published in 2018 at "EBioMedicine"
DOI: 10.1016/j.ebiom.2018.03.014
Abstract: In human pancreatic islets, the neurotransmitter γ-aminobutyric acid (GABA) is an extracellular signaling molecule synthesized by and released from the insulin-secreting β cells. The effective, physiological GABA concentration range within human islets is unknown. Here… read more here.
Keywords: affinity; human pancreatic; gabaa receptors; gaba ... See more keywords
Variations on a scaffold - Novel GABAA receptor modulators.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.07.008
Abstract: Allosteric ligands of GABAA receptors exist in many different chemotypes owing to their great usefulness as therapeutics, with benzodiazepines being among the best known examples. Many allosteric binding sites have been described, among them a… read more here.
Keywords: gabaa receptor; variations scaffold; novel gabaa; gabaa receptors ... See more keywords
Loop‐F of the &agr;‐subunit determines the pharmacologic profile of novel competitive inhibitors of GABAA receptors
Sign Up to like & getrecommendations! Published in 2017 at "European Journal of Pharmacology"
DOI: 10.1016/j.ejphar.2017.01.033
Abstract: ABSTRACT The neurotransmitter &ggr;‐amino butyric acid (GABA) has a fundamental role in CNS function and ionotropic (GABAA) receptors that mediate many of the actions of GABA are important therapeutic targets. This study reports the mechanism… read more here.
Keywords: gabaa receptors; agr subunit; loop agr;
Vasodilatory effects of a variety of positive allosteric modulators of GABAA receptors on rat thoracic aorta.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of pharmacology"
DOI: 10.1016/j.ejphar.2021.174023
Abstract: Different subtypes of GABAA (gamma-aminobutyric acid A) receptors, through their specific regional and cellular localization, are involved in the manifestation of various functions, both at the central and peripheral levels. We hypothesized that various non-neuronal… read more here.
Keywords: thoracic aorta; allosteric modulators; gabaa receptors; rat thoracic ... See more keywords
Arfgef1 haploinsufficiency in mice alters neuronal endosome composition and decreases membrane surface postsynaptic GABAA receptors
Sign Up to like & getrecommendations! Published in 2020 at "Neurobiology of Disease"
DOI: 10.1016/j.nbd.2019.104632
Abstract: ARFGEF1 encodes a guanine exchange factor involved in intracellular vesicle trafficking, and is a candidate gene for childhood genetic epilepsies. To model ARFGEF1 haploinsufficiency observed in a recent Lennox Gastaut Syndrome patient, we studied a… read more here.
Keywords: arfgef1 haploinsufficiency; surface; endosome composition; gabaa receptors ... See more keywords
The Benzodiazepine Binding Sites of GABAA Receptors.
Sign Up to like & getrecommendations! Published in 2018 at "Trends in pharmacological sciences"
DOI: 10.1016/j.tips.2018.03.006
Abstract: 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 GABAA receptors. Benzodiazepines are popular drugs that act as positive… read more here.
Keywords: sites gabaa; benzodiazepine binding; gabaa receptors; binding sites ... See more keywords