AL de Blas, Javier Vitórica, P. Friedrich,
The mAb 62–3G1 to the GABAA receptor/benzodiazepine receptor/Cl- channel complex was used with light-microscopy immunocytochemistry for studying the localization of the GABAA receptors (GABAR) in the rat brain. The results have ... thalamic nucleus, among other areas, were rich in GABAA receptor immunoreactivity. In the cerebellum the granule cell layer ... allowed us to study the distribution of the GABAA receptor with high-resolution light microscopy. These studies have shown that the GABAA receptors are localized in neuronal membranes and concentrated in ...
Tópico(s): Nicotinic Acetylcholine
1988 - Society for Neuroscience | Journal of Neuroscience
L.S. Vedula, Grace Brannigan, Nicoleta J. Economou, Xi Jin, Michael Hall, Renyu Liu, Matthew J. Rossi, William P. Dailey, Kimberly C. Grasty, Michael L. Klein, Roderic G. Eckenhoff, Patrick J. Loll,
... include ligand-gated ion channels such as the GABAA receptor, but such receptor-channel complexes remain challenging to ... able to deal with systems such as the GABAA receptor, it will be necessary to use more tractable ... with the ability to potentiate GABA responses at GABAA receptors, validating this model system for injectable anesthetics. High ... include ligand-gated ion channels such as the GABAA receptor, but such receptor-channel complexes remain challenging to ... able to deal with systems such as the GABAA receptor, it will be necessary to use more tractable ...
Tópico(s): Ion channel regulation and function
2009 - Elsevier BV | Journal of Biological Chemistry
Omar Cauli, Mohammad Taghi Mansouri, Ana Agustí, Vicente Felipo,
... this increase contributes to cognitive impairment.MethodsWe blocked GABAA receptors of rats with bicuculline and analyzed the function ... extracellular GABA; tetrahydrodeoxy-corticosterone (a neurosteroid that enhances GABAA receptor activation); or amounts of the α1, α6, and γ2 subunits of GABAA receptors. The decrease in GABAergic tone observed in the ... could have resulted from the reduced amount of GABAA receptors δ and γ2 subunits or increased levels of pregnanolone (5-fold), which selectively reduces activation of GABAA receptors that contain α4 subunits (widely expressed in cortex ...
Tópico(s): Epilepsy research and treatment
2009 - Elsevier BV | Gastroenterology
Nicholas Graziane, Eunice Y. Yuen, Zhen Yan,
The GABAA receptor-mediated inhibitory transmission in prefrontal cortex (PFC) is implicated in cognitive processes such as working memory. Our ... transport of GABAAR clusters to the surface. The GABAA receptor-mediated inhibitory transmission in prefrontal cortex (PFC) is ... γ-aminobutyric acid; GABAA, GABA, type A; GABAAR, GABAA receptor; ANOVA, analysis of variance; IPSC, inhibitory postsynaptic currents; ... 1822) Google Scholar). GABAergic neurotransmission is mediated by GABAA receptors, the heteropentameric ligand-gated ion channels located at ...
Tópico(s):
2009 - Elsevier BV | Journal of Biological Chemistry
Ayuko Igarashi, Nicole Zadzilka, Machiko Shirahata,
Benzodiazepines (BZs) suppress ventilation possibly by augmenting the GABAA receptor activity in the respiratory control system, but precise ... goals of this study were: (1) to identify GABAA receptor subunits in the carotid body (CB) and petrosal ... test if BZs exert their effects through the GABAA receptor in the CB chemosensory unit. Tissues were taken ... from the brain, and cDNA sequences of several GABAA receptor subunits were determined. Subsequent RT-PCR analysis demonstrated ... and the PG. Immunoreactivity for GABA and for GABAA receptor β3 and γ2 subunits was detected in chemosensory ...
Tópico(s): Sleep and Wakefulness Research
2009 - Springer Nature | Advances in experimental medicine and biology
... potent inhaled (volatile) anaesthetics exhibit positive modulation of GABAA receptors, and also produce significant anaesthesia-compatible effects on ... cyclopropane, nitrous oxide, and xenon, are inactive at GABAA receptors, but block NMDA receptors and activate certain K2P ... represent more potent and specific positive modulators of GABAA receptors, and the i.v. anaesthetic ketamine is a ... Prolongation of synaptic inhibition by modulation of postsynaptic GABAA receptor function at GABAergic synapses is recognized as an ...
Tópico(s): Nicotinic Acetylcholine
2009 - Elsevier BV | British Journal of Anaesthesia
Romy Hoque, Andrew L. Chesson,
... AboutABSTRACTZolpidem is a hypnotic which acts at the GABAA receptor and is indicated for short-term insomnia. Sleep ... benzodiazepine receptor agonists like zolpidem bind to the GABAA receptor at sites that are distinct from the GABA ... neurotransmitters in the mammalian central nervous system (CNS). GABAA receptors exist as pentameric protein complexes, assembled from a ... β, γ, δ, ϵ, θ, and π). Synaptic GABAA receptors are responsible for modulating benzodiazepine sensitivity and typically ... β2 or 3, and the γ2 subunits.6 GABAA receptor sensitivity to benzodiazepines is mediated through α subunits. ...
Tópico(s): Restless Legs Syndrome Research
2009 - American Academy of Sleep Medicine | Journal of Clinical Sleep Medicine
A. Leslie Morrow, James S. Herbert, Pascale Montpied,
... and inverse agonist effects on the function of GABAA receptor-gated Cl− channels in the central nervous system ( ... that prolonged ethanol inhalation reduces the expression of GABAA receptor α1 and α2 subunit mRNAs in the rat ... for 2 weeks using a pair-fed design. GABAA receptor α subunit mRNA levels were quantified by Northern analysis using specific cRNA probes. GABAA receptor α1 subunit mRNA levels were reduced in the ... cerebellum, chronic ethanol ingestion reduced the levels of GABAA receptor α1 subunit mRNAs (4.8 and 4.4 ...
Tópico(s): Biochemical Analysis and Sensing Techniques
1992 - Elsevier BV | Molecular and Cellular Neuroscience
Mike Beck, Kieran Brickley, Helen Wilkinson, Seema Sharma, Miriam J. Smith, Paul L. Chazot, Simon Pollard, F. Anne Stephenson,
... amino acid protein, γ-aminobutyric acid type A (GABAA) receptor interacting factor-1 (GRIF-1), has been cloned ... by virtue of its specific interaction with the GABAA receptor β2 subunit intracellular loop in a yeast two- ... kDa. Co-expression of GRIF-1a and α1β2γ2 GABAA receptors in mammalian cells revealed some co-localization in ... GRIF-1-(8–633) specifically precipitated in vitro GABAA receptor α1 and β2 subunit immunoreactivities from detergent extracts of adult rat brain. The respective GABAA receptor β2 subunit/GRIF-1 binding domains were mapped ...
Tópico(s): Neuropeptides and Animal Physiology
2002 - Elsevier BV | Journal of Biological Chemistry
Gregory W. Sawyer, David C. Chiara, Richard W. Olsen, Jonathan B. Cohen,
... binding site in γ-aminobutyric acid type A (GABAA) receptors may allosterically modulate function. Depending upon the ligand, ... and/or allosteric coupling have been identified within GABAA receptor α and γ subunits that localize the binding ... α1Tyr-210, α2Tyr-209, and α3Tyr-234, in GABAA receptors containing those subunits. These results are discussed in ... binding site in γ-aminobutyric acid type A (GABAA) receptors may allosterically modulate function. Depending upon the ligand, ... and/or allosteric coupling have been identified within GABAA receptor α and γ subunits that localize the binding ...
Tópico(s): Neurotransmitter
2002 - Elsevier BV | Journal of Biological Chemistry
Sabine W. Baumann, Roland Baur, Erwin Sigel,
... isoform of the γ-aminobutyric acid type A (GABAA) receptor is thought to be composed of 2α1, 2β2, ... subunit arrangement is lacking. We show here that GABAA receptor subunits can be concatenated to a trimer that ... isoform of the γ-aminobutyric acid type A (GABAA) receptor is thought to be composed of 2α1, 2β2, ... subunit arrangement is lacking. We show here that GABAA receptor subunits can be concatenated to a trimer that ... Google Scholar). The major receptor isoform of the GABAA receptor in the brain most probably consists of α1, ...
Tópico(s): Ion channel regulation and function
2002 - Elsevier BV | Journal of Biological Chemistry
Mohammed Dibas, Eric B. Gonzales, Paromita Das, Cathy L. Bell-Horner, Glenn H. Dillon,
... reciprocal mutation in the β2 subunit of α1β2 GABAA receptors (α1β2(N15′S) receptors) decreased the magnitude of ... reciprocal mutation in the β2 subunit of α1β2 GABAA receptors (α1β2(N15′S) receptors) decreased the magnitude of ... PubMed Scopus (22) Google Scholar), picrotoxin inhibition of GABAA receptors and glutamate-gated Cl− channels is strongly use- ... affects the mechanism of the picrotoxin blockade in GABAA receptors, because receptors expressing the reciprocal mutation (N15′S) in the β2 subunit of α1β2 GABAA receptors displayed significantly less use-facilitated block than observed ...
Tópico(s): Epilepsy research and treatment
2002 - Elsevier BV | Journal of Biological Chemistry
Ratnakumari Lingamaneni, Hugh C. Hemmings,
... 35S]TBPS) binding to the picrotoxinin site of GABAA receptors, [3H]batrachotoxinin A 20-α benzoate ([3H]BTX- ... target set. I.V. anaesthetics interacted preferentially with GABAA receptors, while volatile anaesthetics were essentially equipotent at Na+ channels and GABAA receptors. Antiepileptic drugs could be classified by preferential actions at either Na+ channels or GABAA receptors. Anaesthetics and antiepileptic drugs have agent-specific effects ... and antiepileptic drugs interact with Na+ channels and GABAA receptors at therapeutic concentrations, in most cases with little ...
Tópico(s): Epilepsy research and treatment
2003 - Elsevier BV | British Journal of Anaesthesia
Ramin Darbandi-Tonkabon, William R. Hastings, Chun‐min Zeng, Gustav Akk, Brad D. Manion, John Bracamontes, Joseph H. Steinbach, Steven Mennerick, Douglas F. Covey, Alex S. Evers,
... the function of γ-aminobutyric acid, type A (GABAA) receptors in the central nervous system by an unknown ... brain. 6-AziP is an effective modulator of GABAA receptors as evidenced by its ability to inhibit binding ... oocytes and human endothelial kidney 293 cells expressing GABAA receptor subunits (α1β2γ2). [3H]6-AziP produced time- and ... 6-AziP. The β2and β3 subunits of the GABAA receptor were co-immunoprecipitated by the VDAC-1 antibody suggesting a physical association between VDAC-1 and GABAA receptors in rat brain membranes. These data suggest that ...
Tópico(s): Ion channel regulation and function
2003 - Elsevier BV | Journal of Biological Chemistry
Yoshito Mizoguchi, Takashi Kanematsu, Masato Hirata, Junichi Nabekura,
... number of postsynaptic γ-aminobutyric acid type A (GABAA) receptors is a fundamental determinant of the variability of ... increase in the total number of cell surface GABAA receptors, through the activation of Trk B receptor tyrosine ... that BDNF rapidly induced a sustained potentiation of GABAA receptor-mediated currents, using nystatin-perforated patch clamp recordings, ... in the total number of cell surface functional GABAA receptors in visual cortical pyramidal neurons. These results suggest ... BDNF could alter the number of cell surface GABAA receptors in a region-specific manner. The number of ...
Tópico(s): Neurogenesis and neuroplasticity mechanisms
2003 - Elsevier BV | Journal of Biological Chemistry
A. Christine Engblom, Flemming Fryd Johansen, Uffe Kristiansen,
... of mRNA for γ-aminobutyric acid type A (GABAA) receptor α1–6, औ1–3, γ1–3, and δ ... of mRNA for γ-aminobutyric acid type A (GABAA) receptor α1–6, औ1–3, γ1–3, and δ ... 113-159Crossref PubMed Scopus (412) Google Scholar). The GABAA receptor subunits are expressed in a region- and age- ... Google Scholar). Knowledge of the distribution of different GABAA receptor subtypes, both anatomically and developmentally, is therefore essential ... pharmacological actions of drugs that act on different GABAA receptor subtypes. Cerebellar granule neurons are used for studying ...
Tópico(s): Lipid Membrane Structure and Behavior
2003 - Elsevier BV | Journal of Biological Chemistry
Rachel F. Tyndale, T. G. Hales, RW Olsen, AJ Tobin,
We have investigated the GABAA receptor mRNA composition in 13 cell lines, using 13 subunit-specific oligo-primers (alpha 1-6, beta 1-3, gamma 1- ... order to identify homogeneous cellular sources with distinctive GABAA receptor subunits. Fifteen GABAA receptor subunits have been cloned from mammalian tissue (those ... rho 1 and rho 2). This multiplicity of GABAA receptor subunits underlies the diverse pharmacology of the GABAA receptor. Attempts to understand the regulation and pharmacology of ... a lack of pure populations of cells expressing GABAA receptor subunits. Permanent cell lines provide such a resource. ...
Tópico(s):
1994 - Society for Neuroscience | Journal of Neuroscience
Wendy J. Keir, A. Leslie Morrow,
... suggest an important role for ethanol interactions with GABAA receptors in the development of the ethanol withdrawal syndrome. ... withdrawal seizure severity and the expression of particular GABAA receptor subunits in mouse lines selectively bred for differential sensitivity to ethanol withdrawal seizures. Since GABAA receptor subunit levels are subject to modulation by ethanol, the levels of GABAA receptor α1, α6 and β2 subunit mRNAs were measured ... from groups of 6–10 animals and the GABAA receptor subunit mRNA levels were quantified by Northern blot ...
Tópico(s): Parkinson's Disease Mechanisms and Treatments
1994 - Elsevier BV | Molecular Brain Research
Hideaki Okumichi, Mina Mizukami, Yoshiaki Kiuchi, Takashi Kanamoto,
... that the expression of the protein of the GABAA receptor β1 subunit was significantly increased in the retina ... study was to investigate the role played by GABAA receptor β1 subunit in the death of retinal ganglion ... stress. The retinal sites and expression pattern of GABAA receptor β1 subunit were determined by immunohistochemistry in the ... A RGC line, RGC-5, was exposed to GABAA receptor agonist and antagonist, and the cell viability was determined by the MTS assay. The effect of GABAA receptor antagonist on the death of RGCs, and the ...
Tópico(s): Nicotinic Acetylcholine
2008 - Elsevier BV | Experimental Eye Research
... it mediates fast inhibition by activating synaptic ionotropic GABAA receptors. GABAA receptors are pentamers constructed from a possible 16 subunits ( ... determined the subunit composition of synaptic and extrasynaptic GABAA receptors in dentate gyrus granule cells (Fig. 1). Dentate ... 2003). Previous work has established the involvement of GABAA receptors containing α4 and δ subunits, which confer high ... hippocampal pyramidal cells, in which more than one GABAA receptor subtype contributes to the tonic current (Scimemi et ...
Tópico(s): Pharmacological
2008 - Wiley | The Journal of Physiology
Kun Xiang, Elizabeth I. Tietz,
... flurazepam (FZP) administration in rats results in reduced GABAA receptor-mediated synaptic transmission in CA1 pyramidal neurons associated ... in regulating benzodiazepine-induced changes in CA1 neuron GABAA receptor-mediated function was evaluated. Nimodipine (10 mg/kg, ... in vitro tolerance to zolpidem. The reduction in GABAA receptor-mediated mIPSC amplitude and estimated unitary channel conductance ... suggesting multiple mechanisms may be involved in regulating GABAA receptor-mediated synaptic transmission following chronic FZP administration. As ...
Tópico(s): Neural dynamics and brain function
2008 - Elsevier BV | Neuroscience
Arunesh Saras, Günter Gisselmann, Angela K. Vogt-Eisele, Katja S. Erlkamp, Olaf Kletke, H. Pusch, Hanns Hatt,
... vertebrate ion channels and identified β subunits of GABAA receptors as potential candidates for histamine-gated channels. In ... Despite the vast number of synthetic modulators of GABAA receptors widely used in medicine, which act on several ... for the first time that histamine modulates heteromultimeric GABAA receptors and may thus represent an endogenous ligand for ... vertebrate ion channels and identified β subunits of GABAA receptors as potential candidates for histamine-gated channels. In ... Despite the vast number of synthetic modulators of GABAA receptors widely used in medicine, which act on several ...
Tópico(s):
2008 - Elsevier BV | Journal of Biological Chemistry
... major subtypes of the GABA receptor exist: the GABAA receptor is a pentameric, chloride ionophore that primarily mediates ... sympatho-excitatory responses induced by the microinjection of GABAA receptor agonists were no different comparing normotensive rats to ... in function, found that the ability of the GABAA receptor agonist muscimol to inhibit aortic nerve (baroreceptor) evoked ... desensitization of GABAA evoked responses. The alterations in GABAA receptor-evoked currents are consistent with the in vivo ...
Tópico(s): Nicotinic Acetylcholine
2010 - Lippincott Williams & Wilkins | Hypertension
... brain. Its fast inhibitory actions are mediated by GABAA receptors representing ligand-operated chloride channels. GABAA receptors consist of 5 subunits generally belonging to different ... Olsen, 1994). Molecular cloning of complementary DNA encoding GABAA receptors in humans identified 8 different subunit classes with ... indicating formation of a large number of different GABAA receptor subtypes with distinct subunit composition (For review, see Sieghart and Sperk, 2002). GABAA receptors are the site of action of several antiepileptic ...
Tópico(s): DNA and Nucleic Acid Chemistry
2007 - Wiley | Epilepsia
Charlotte D’Hulst, R. Frank Kooy,
GABAA receptors are the major inhibitory neurotransmitter receptors in the mammalian brain, implicated in anxiety, depression, epilepsy, insomnia, ... of the GABAergic system, and in particular the GABAA receptor-mediated function, in fragile X syndrome, the most ... We argue that an altered expression of the GABAA receptor has neurophysiologic and functional consequences that might relate ... treated with therapeutic agents that act on the GABAA receptor. Therefore, the GABAA receptor might be a novel therapeutic target for fragile ...
Tópico(s): Autism Spectrum Disorder Research
2007 - Elsevier BV | Trends in Neurosciences
Janardhan P. Bhattarai, Seon Ah Park, Jin Bong Park, So Yeong Lee, Allan E. Herbison, Pan Dong Ryu, Seong Kyu Han,
Abstract It is well established that the GABAA receptor plays an important role in regulating the electrical excitability of GnRH neurons. Two different modes of GABAA receptor signaling exist: one mediated by synaptic receptors generating ... extrasynaptic receptors generating a persistent (tonic) current. Using GABAA receptor antagonists picrotoxin, bicuculline methiodide, and gabazine, which differentiate ... GnRH neurons exhibit an approximately 15-pA tonic GABAA receptor current in the acute brain slice preparation. The ...
Tópico(s): Neurogenesis and neuroplasticity mechanisms
2011 - Oxford University Press | Endocrinology
Dong Hyun Kim, Jong‐Min Kim, Se Jin Park, Seungheon Lee, Chan Young Shin, Jae Hoon Cheong, Jong Hoon Ryu,
... suggests that the γ-aminobutyric acid type A (GABAA) receptor has a crucial role in memory retrieval. However, the signaling mechanisms underlying the role of GABAA receptor modulation in memory retrieval are unclear. We conducted ... in the hippocampus to test the effects of GABAA receptor modulation on memory retrieval. We further tested the ... retrieval during the task. Accordingly, to investigate whether GABAA receptor activation or inhibition induces ERK phosphorylation during memory retrieval, drugs that target the GABAA receptor were administered into the hippocampus before the retention ...
Tópico(s): Neuroinflammation and Neurodegeneration Mechanisms
2011 - Springer Nature | Neuropsychopharmacology
S P H Alexander, Alistair Mathie, JA Peters,
... Macdonald RL, Walker MC, Cope DW (2009). Extrasynaptic GABAA receptors: form, pharmacology, and function. J Neurosci29: 12757–12763. ... acetylcholine receptors. IUBMB Life61: 407–423. Overview: The GABAA receptor is a ligand-gated ion channel of the ... acetylcholine, 5-HT3 and strychnine-sensitive glycine receptors. GABAA receptor-mediated inhibition within the CNS occurs by fast ... been termed ‘GABAA, slow’ (Campogna and Pearce, 2011). GABAA receptors exist as pentamers of 4TM subunits that form ... ρ, one ε, one π and one θ GABAA receptor subunits (Ensembl gene family ID ENSF00000000053) have been ...
Tópico(s):
2011 - Wiley | British Journal of Pharmacology
Daniel W. Wheeler, Andrew J. Thompson, Federico Corletto, Jill Reckless, Justin Loke, Nicolas Lapaque, Andrew J. Grant, Pietro Mastroeni, David J. Grainger, Claire L. Padgett, John O’Brien, Nigel Miller, John Trowsdale, Sarah C. R. Lummis, David Menon, John S. Beech,
Background GABAA receptors are members of the Cys-loop family of neurotransmitter receptors, proteins which are responsible for fast synaptic ... die [3]–[6]. As many anaesthetics act via GABAA receptors [7], the aim of this study was to ... We demonstrate, using RT-PCR, that monocytes express GABAA receptors constructed of α1, α4, β2, γ1 and/or ... chloride-selective channel; activation is inhibited by the GABAA receptor antagonists bicuculline and picrotoxin, but not enhanced by ... drugs propofol and thiopental, which can act via GABAA receptors, impaired monocyte function in classic immunological chemotaxis and ...
Tópico(s): Neuroscience and Neuropharmacology Research
2011 - Public Library of Science | PLoS ONE
Takashi Kanematsu, Atsushi Yasunaga, Yoshito Mizoguchi, Akiko Kuratani, Josef T. Kittler, Jasmina N. Jovanovic, Kei Takenaka, Keiichi I. Nakayama, Kiyoko Fukami, Tadaomi Takenawa, Stephen J. Moss, Junichi Nabekura, Masato Hirata,
... GABAergic transmission. Exposure to BDNF alters properties of GABAA receptors and induces changes in the expression level at ... 1 (PRIP-1) plays an important role in GABAA receptor trafficking and function, its role in BDNF-dependent ... correlated with a gradual increase in phosphorylation of GABAA receptor β3 subunit in response to BDNF. To characterize ... examined the recruitment of protein phosphatase(s) to GABAA receptors. We demonstrate that PRIP associates with phosphatases as ... β subunits. PRIP was found to colocalize with GABAA receptor clusters in cultured neurons and with recombinant GABAA ...
Tópico(s): Ion channel regulation and function
2006 - Elsevier BV | Journal of Biological Chemistry