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Zhi-Ao Chen et al.
Cancer biology & medicine, 9(2), 90-98 (2013-05-22)
To investigate the roles of the γ-aminobutyric acid (GABA) in the metastasis of hepatocellular carcinoma (HCC) and to explore the potential of a novel therapeutic approach for the treatment of HCC. The expression levels of GABA receptor subunit genes in
Stephanie Rudolph et al.
Cell reports, 33(5), 108338-108338 (2020-11-05)
Granule cells (GCs) of the cerebellar input layer express high-affinity δ GABAA subunit-containing GABAA receptors (δGABAARs) that respond to ambient GABA levels and context-dependent neuromodulators like steroids. We find that GC-specific deletion of δGABAA (cerebellar [cb] δ knockout [KO]) decreases
Yuya Ogawa et al.
Pharmacology, biochemistry, and behavior, 198, 173034-173034 (2020-09-11)
In the spinal cord, γ-aminobutyric acid (GABA) interneurons play an essential role in antinociception. However, not all actions of GABA favor antinociception at the supraspinal level. We previously reported that gabaculine, which increases endogenous GABA in the synaptic clefts, induces
Zhiwen Ye et al.
Frontiers in neural circuits, 7, 203-203 (2014-01-07)
We have made use of the δ subunit-selective allosteric modulator DS2 (4-chloro-N-[2-(2-thienyl)imidazo[1,2-a]pyridine-3-yl benzamide) to assay the contribution of δ-GABAARs to tonic and phasic conductance changes in the cerebellum, thalamus and neocortex. In cerebellar granule cells, an enhancement of the tonic
Marcia J Ramaker et al.
Psychopharmacology, 232(8), 1415-1426 (2014-10-25)
Allopregnanolone (ALLO) is an endogenous neuroactive steroid thought to alter the reinforcement value of alcohol (ethanol) due to its actions as a positive modulator of the GABAA receptor (GABAAR). Extrasynaptic GABAARs may be a particularly sensitive target of ethanol and
Yasuyuki Nagumo et al.
Cell reports, 31(12), 107797-107797 (2020-06-25)
Peripheral nerve injury induces functional and structural remodeling of neural circuits along the somatosensory pathways, forming the basis for somatotopic reorganization and ectopic sensations, such as referred phantom pain. However, the mechanisms underlying that remodeling remain largely unknown. Whisker sensory
GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic.
Krogsgaard-Larsen P, et al.
Biochemical Pharmacology, 68(8), 1573-1580 (2004)
Chemistry and pharmacology of the GABA agonists THIP (Gaboxadol) and isoguvacine.
Krogsgaard-Larsen, et al.
Drugs of the Future, 9, 597-618 (1984)
Nora Siegal Silverman et al.
Experimental and clinical psychopharmacology, 24(2), 131-141 (2016-02-24)
Behavioral sensitization to psychostimulants is associated with changes in dopamine (DA), glutamate, and GABA within the mesocorticolimbic and nigrostriatal DA systems. Because GABAA receptors are highly expressed within these systems, we examined the role of these receptors containing a δ
Christina B Falk-Petersen et al.
Basic & clinical pharmacology & toxicology, 121(2), 119-129 (2017-03-17)
δ-Containing GABAA receptors are located extrasynaptically and mediate tonic inhibition. Their involvement in brain physiology positions them as interesting drug targets. There is thus a continued interest in establishing reliable recombinant expression systems for δ-containing GABAA receptors. Inconveniently, the recombinant
P Krogsgaard-Larsen et al.
Journal of medicinal chemistry, 26(6), 895-900 (1983-06-01)
The thio analogues of the GABA (gamma-aminobutyric acid) agonist THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol), the GABA uptake inhibitor THPO (4,5,6,7-tetrahydroisoxazolo[4,5-c]pyridin-3-ol), and the glycine antagonist THAZ (5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol) have been synthesized and tested biologically on single neurons in the cat spinal cord and in vitro
Suppression of Human Liver Cancer Cell Migration and Invasion via the GABAA Receptor
Chen ZA, et al.
Cancer Biology & Medicine, 9(2), 90-90 (2012)
Jeffery A Boychuk et al.
Experimental neurology, 277, 178-189 (2016-01-17)
Changes in functional GABAAR signaling in hippocampus have previously been evaluated using pre-clinical animal models of either diffuse brain injury or extreme focal brain injury that precludes measurement of cells located ipsilateral to injury. As a result, there is little
Tissue transglutaminase and its role in human cancer progression.
Bo Li et al.
Advances in enzymology and related areas of molecular biology, 78, 247-293 (2012-01-10)
GABA Site Agonist Gaboxadol Induces Addiction-Predicting Persistent Changes in Ventral Tegmental Area Dopamine Neurons But Is Not Rewarding in Mice or Baboons
Vashchinkina E, et al.
The Journal of Neuroscience, 32(15), 5310-5320 (2012)
TEXTBOOK OF GERIATRIC MEDICINE INTERNATIONAL (2011)
Chang Liu et al.
Current biology : CB, 29(21), 3635-3646 (2019-11-02)
Both the structure and the amount of sleep are important for brain function. Entry into deep, restorative stages of sleep is time dependent; short sleep bouts selectively eliminate these states. Fragmentation-induced cognitive dysfunction is a feature of many common human
Mariah A A Meyer et al.
Learning & memory (Cold Spring Harbor, N.Y.), 24(9), 385-391 (2017-08-18)
Retrieval of fear memories can be state-dependent, meaning that they are best retrieved if the brain states at encoding and retrieval are similar. Such states can be induced by activating extrasynaptic γ-aminobutyric acid type A receptors (GABA
Matthew V Green et al.
Neuropharmacology, 149, 161-168 (2019-02-24)
HIV-Associated Neurocognitive disorder (HAND) affects nearly half of infected patients. The HIV envelope protein gp120 is shed by infected cells and is a potent neurotoxin in vitro that reproduces many aspects of HAND when expressed in vivo. Here, we show
Maya A Rhine et al.
Autism research : official journal of the International Society for Autism Research, 12(3), 401-421 (2019-01-18)
Autism spectrum disorder is a neurodevelopmental syndrome diagnosed primarily by persistent deficits in social interactions and communication, unusual sensory reactivity, motor stereotypies, repetitive behaviors, and restricted interests. No FDA-approved medical treatments exist for the diagnostic symptoms of autism. Here we
Joseph L Bedont et al.
eLife, 10 (2021-06-05)
Sleep is a conserved and essential behavior, but its mechanistic and functional underpinnings remain poorly defined. Through unbiased genetic screening in Drosophila, we discovered a novel short-sleep mutant we named argus. Positional cloning and subsequent complementation, CRISPR/Cas9 knock-out, and RNAi
Sarah H Hayes et al.
Progress in neurobiology, 196, 101893-101893 (2020-08-14)
Various theories and their associated mechanisms have been proposed as the neural basis of phantom sound perception (tinnitus), including central gain enhancement and altered cortical oscillations. However, it remains unknown whether these cortical changes directly cause tinnitus, or simply coexist
Vanessa M Hill et al.
PLoS biology, 16(7), e2005206-e2005206 (2018-07-13)
Although sleep appears to be broadly conserved in animals, the physiological functions of sleep remain unclear. In this study, we sought to identify a physiological defect common to a diverse group of short-sleeping Drosophila mutants, which might provide insight into
GABA and Sleep: Molecular, Functional and Clinical Aspects (2010)
Mohsen Seifi et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 34(31), 10361-10378 (2014-08-01)
The enteric nervous system (ENS) provides the intrinsic neural control of the gastrointestinal tract (GIT) and regulates virtually all GI functions. Altered neuronal activity within the ENS underlies various GI disorders with stress being a key contributing factor. Thus, elucidating
M Lancel
Sleep, 22(1), 33-42 (1999-02-16)
This paper reviews the sleep effects of systemically administered agonistic modulators of GABAA receptors, including barbiturates, benzodiazepines, zolpidem, zopiclone and neuroactive steroids, and the selective GABAA agonists muscimol and THIP. To assess the involvement of GABAA receptors in the physiologic
M C Chakrabarti et al.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 37(8), 1384-1388 (1996-08-01)
Monoclonal antibody may undergo loss of immunoreactivity due to radiation damage when labeled with large amounts of 131I or 90Y for therapy. Our aim was to develop a method to protect an antibody during the labeling procedure. As a model
Qian Wang et al.
Nature communications, 11(1), 679-679 (2020-02-06)
Auxin determines the developmental fate of plant tissues, and local auxin concentration is precisely controlled. The role of auxin transport in modulating local auxin concentration has been widely studied but the regulation of local auxin biosynthesis is less well understood.
Xing Feng et al.
Autophagy, 1-20 (2020-03-19)
Although the treatment of brain tumors by targeting kinase-regulated macroautophagy/autophagy, is under investigation, the precise mechanism underlying autophagy initiation and its significance in glioblastoma (GBM) remains to be defined. Here, we report that PAK1 (p21 [RAC1] activated kinase 1) is
Xi Zhang et al.
Plant physiology, 181(2), 480-498 (2019-08-23)
The dual-affinity nitrate transceptor NITRATE TRANSPORTER1.1 (NRT1.1) has two modes of transport and signaling, governed by Thr-101 (T101) phosphorylation. NRT1.1 regulates lateral root (LR) development by modulating nitrate-dependent basipetal auxin export and nitrate-mediated signal transduction. Here, using the Arabidopsis (Arabidopsis
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