Results 21 to 30 of about 39,325 (214)

Novel Molecule Exhibiting Selective Affinity for GABAA Receptor Subtypes

open access: yesScientific Reports, 2017
Aminoquinoline derivatives were evaluated against a panel of receptors/channels/transporters in radioligand binding experiments. One of these derivatives (DCUK-OEt) displayed micromolar affinity for brain γ-aminobutyric acid type A (GABAA) receptors ...
Cecilia M. Borghese   +10 more
doaj   +1 more source

Increased motor-impairing effects of the neuroactive steroid pregnanolone in mice with targeted inactivation of the GABAA receptor gamma2 subunit in the cerebellum

open access: yesFrontiers in Pharmacology, 2016
Endogenous neurosteroids and neuroactive steroids have potent and widespread actions on the brain via inhibitory GABAA receptors. In recombinant receptors and genetic mouse models their actions depend on the alpha, beta and delta subunits of the receptor,
Elli Leppä   +8 more
doaj   +1 more source

Knockdown of GABAA alpha3 subunits on thalamic reticular neurons enhances deep sleep in mice

open access: yesNature Communications, 2022
Uygun et al. show that deletion of GABAA receptors from the thalamic reticular nucleus using CRISPR gene editing in mice boosts the delta waves, indicating a role for GABAA receptors on thalamic reticular nucleus neurons in NREM sleep delta oscillations.
David S. Uygun   +8 more
doaj   +1 more source

Positron Emission Tomography (PET) Quantification of GABAA Receptors in the Brain of Fragile X Patients. [PDF]

open access: yesPLoS ONE, 2015
Over the last several years, evidence has accumulated that the GABAA receptor is compromised in animal models for fragile X syndrome (FXS), a common hereditary form of intellectual disability.
Charlotte D'Hulst   +11 more
doaj   +1 more source

Disrupted GABAAR trafficking and synaptic inhibition in a mouse model of Huntington's disease

open access: yesNeurobiology of Disease, 2012
Growing evidence suggests that Huntington's disease (HD), a neurodegenerative movement disorder caused by the mutant huntingtin (htt) with an expanded polyglutamine (polyQ) repeat, is associated with the altered intracellular trafficking and synaptic ...
Eunice Y. Yuen   +3 more
doaj   +1 more source

Role of GABA receptors in fetal lung development in rats. [PDF]

open access: yesPLoS ONE, 2010
Fluid accumulation is critical for lung distension and normal development. The multi-subunit γ-amino butyric acid type A receptors (GABAA) mainly act by mediating chloride ion (Cl-) fluxes.
Narendranath Reddy Chintagari   +5 more
doaj   +1 more source

γ-Hydroxybutyric acid (GHB) is not an agonist of extrasynaptic GABAA receptors. [PDF]

open access: yesPLoS ONE, 2013
γ-Hydroxybutyric acid (GHB) is an endogenous compound and a drug used clinically to treat the symptoms of narcolepsy. GHB is known to be an agonist of GABAB receptors with millimolar affinity, but also binds with much higher affinity to another site ...
William M Connelly   +2 more
doaj   +1 more source

Gephyrin, the enigmatic organizer at GABAergic synapses

open access: yesFrontiers in Cellular Neuroscience, 2012
GABAA receptors are clustered at synaptic sites to achieve a high density of postsynaptic receptors opposite the input axonal terminals. This allows an efficient propagation of GABA mediated signals, which mostly result in neuronal inhibition.
Verena Eva Tretter   +5 more
doaj   +1 more source

Unraveling 4‐Phenylbutyrate's Therapeutic Role in SLC6A1 Disorders: Pharmacochaperoning Over HDAC Inhibition

open access: yesAnnals of Clinical and Translational Neurology, EarlyView.
ABSTRACT Objective Variants in SLC6A1, encoding the GABA transporter 1 (GAT‐1), cause epilepsy, autism spectrum disorder, and developmental delay via loss of GABA uptake, impaired trafficking, and ER retention. We previously found that 4‐Phenylbutyrate (PBA), an FDA‐approved drug, restores GABA uptake and reduces seizures in SLC6A1‐related disorders ...
Melissa B. DeLeeuw   +5 more
wiley   +1 more source

MUSCARINIC LONG-TERM ENHANCEMENT OF TONIC AND PHASIC GABAA INHIBITION IN RAT CA1 PYRAMIDAL NEURONS

open access: yesFrontiers in Cellular Neuroscience, 2016
Acetylcholine (ACh) regulates network operation in the hippocampus by controlling excitation and inhibition in rat CA1 pyramidal neurons (PCs), the latter through gamma-aminobutyric acid type-A receptors (GABAARs).
Soledad Dominguez   +2 more
doaj   +1 more source

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